Konstantinović, Jelena M.

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Authority KeyName Variants
orcid::0000-0002-2572-8538
  • Konstantinović, Jelena M. (16)
  • Konstantinović, Jelena (2)
Projects
The synthesis of aminoquinoline-based antimalarials and botulinum neurotoxin A inhibitors Control of infections by Apicomplexan pathogens: from novel drug targets to prediction
Serbian Academy of Sciences and Arts Ministero dellIstruzione, dellUniversita e della Ricerca (PRIN) Project [20154JRJPP_004]
Serbian Academy of Sciences and Arts, Executive Programme of Scientific and Technological Cooperation between the Italian Republic and the Republic of Serbia Bill & Melinda Gates Foundation [OPP1040394]
Fundacao para a Ciencia e Tecnologia, Portugal [PTDC/SAUMIC/117060/2010] Reinforcement of the Faculty of Chemistry, University of Belgrade, towards becoming a Center of Excellence in the region of WB for Molecular Biotechnology and Food research
Rational design and synthesis of biologically active and coordination compounds and functional materials, relevant for (bio)nanotechnology Microbial diversity study and characterization of beneficial environmental microorganisms
National Institute of Allergy and Infectious Diseases (U.S.) [5-U01AI082051-02, R33-AI101387] Serbian Academy of Sciences and Arts [F80]
University of Milan “Piano sostegno alla Ricerca, Linea 2 2018" U.S. Defense Threat Reduction Agency/Joint Science and Technology Office
Ministero dell’Istruzione, dell’Universit a e della Ricerca [PRIN 2015.4JRJPP_004] Ministero dell’Istruzione, dell’Universit a e della Ricerca [PRIN 2015.4JRJPP_004]
National Cancer Institute, National Institutes of Health (U.S.) [HHSN261200800001E] National Institute of Allergy and Infectious Diseases (U.S.) [5-U01AI082051-02]
Serbian Academy of Sciences and Arts (BS, Grant F80) Serbian Academy of Sciences and Arts (BS, Grant F80)
Spanish Ministerio de Ciencia, Innovacion y Universidades Grant (RTI2018-097210-B-I00 to FG) Spanish Ministerio de Ciencia, Innovacion y Universidades Grant (RTI2018-097210-B-I00 to FG).

Author's Bibliography

4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania

Manzano, Jose Ignacio; Konstantinović, Jelena; Scaccabarozzi, Diletta; Perea, Ana; Pavić, Aleksandar; Cavicchini, Loredana; Basilico, Nicoletta; Gamarro, Francisco; Šolaja, Bogdan A.

(Elsevier, 2019)

TY  - JOUR
AU  - Manzano, Jose Ignacio
AU  - Konstantinović, Jelena
AU  - Scaccabarozzi, Diletta
AU  - Perea, Ana
AU  - Pavić, Aleksandar
AU  - Cavicchini, Loredana
AU  - Basilico, Nicoletta
AU  - Gamarro, Francisco
AU  - Šolaja, Bogdan A.
PY  - 2019
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/3287
AB  - Among neglected tropical diseases, leishmaniasis is one of the most relevant with an estimated 30,000 deaths annually. Existing therapies have serious drawbacks in safety, drug resistance, field-adapted application and cost; therefore, new safer and shorter treatments are needed for this disease. Here we report on the synthesis of novel 4-amino-7-chloroquinoline-based compounds with leishmanicidal activity, together with deeper insight into the mechanism of action of our previously published hit compound 1. New derivatives showed comparable activity to 1 against both promastigote and intracellular amastigote forms of Leishmania infantum, with IC50 < 1 mM. Furthermore, we have determined that compound 1 induced a decrease of intracellular ATP levels, as well as a mitochondrial depolarization, together with an alteration of plasma membrane permeability and a significant ROS production. The inhibition of the energy metabolism of Leishmania plays an important role in the leishmanicidal mechanism of this compound. In all, these results support the consideration of compound 1 for the future development of new leishmanicidal drugs.
PB  - Elsevier
T2  - European Journal of Medicinal Chemistry
T1  - 4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania
VL  - 180
SP  - 28
EP  - 40
DO  - 10.1016/j.ejmech.2019.07.010
ER  - 
@article{
author = "Manzano, Jose Ignacio and Konstantinović, Jelena and Scaccabarozzi, Diletta and Perea, Ana and Pavić, Aleksandar and Cavicchini, Loredana and Basilico, Nicoletta and Gamarro, Francisco and Šolaja, Bogdan A.",
year = "2019",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/3287",
abstract = "Among neglected tropical diseases, leishmaniasis is one of the most relevant with an estimated 30,000 deaths annually. Existing therapies have serious drawbacks in safety, drug resistance, field-adapted application and cost; therefore, new safer and shorter treatments are needed for this disease. Here we report on the synthesis of novel 4-amino-7-chloroquinoline-based compounds with leishmanicidal activity, together with deeper insight into the mechanism of action of our previously published hit compound 1. New derivatives showed comparable activity to 1 against both promastigote and intracellular amastigote forms of Leishmania infantum, with IC50 < 1 mM. Furthermore, we have determined that compound 1 induced a decrease of intracellular ATP levels, as well as a mitochondrial depolarization, together with an alteration of plasma membrane permeability and a significant ROS production. The inhibition of the energy metabolism of Leishmania plays an important role in the leishmanicidal mechanism of this compound. In all, these results support the consideration of compound 1 for the future development of new leishmanicidal drugs.",
publisher = "Elsevier",
journal = "European Journal of Medicinal Chemistry",
title = "4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania",
volume = "180",
pages = "28-40",
doi = "10.1016/j.ejmech.2019.07.010"
}
Manzano, J. I., Konstantinović, J., Scaccabarozzi, D., Perea, A., Pavić, A., Cavicchini, L., Basilico, N., Gamarro, F.,& Šolaja, B. A. (2019). 4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania.
European Journal of Medicinal Chemistry
Elsevier., 180, 28-40.
https://doi.org/10.1016/j.ejmech.2019.07.010
Manzano JI, Konstantinović J, Scaccabarozzi D, Perea A, Pavić A, Cavicchini L, Basilico N, Gamarro F, Šolaja BA. 4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania. European Journal of Medicinal Chemistry. 2019;180:28-40
Manzano Jose Ignacio, Konstantinović Jelena, Scaccabarozzi Diletta, Perea Ana, Pavić Aleksandar, Cavicchini Loredana, Basilico Nicoletta, Gamarro Francisco, Šolaja Bogdan A., "4-Aminoquinoline-based compounds as antileishmanial agents that inhibit the energy metabolism of Leishmania" European Journal of Medicinal Chemistry, 180 (2019):28-40,
https://doi.org/10.1016/j.ejmech.2019.07.010 .
1
3
4
4

Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010

Manzano, Jose Ignacio; Konstantinović, Jelena; Scaccabarozzi, Diletta; Perea, Ana; Pavić, Aleksandar; Cavicchini, Loredana; Basilico, Nicoletta; Gamarro, Francisco; Šolaja, Bogdan A.

(Elsevier, 2019)

TY  - BOOK
AU  - Manzano, Jose Ignacio
AU  - Konstantinović, Jelena
AU  - Scaccabarozzi, Diletta
AU  - Perea, Ana
AU  - Pavić, Aleksandar
AU  - Cavicchini, Loredana
AU  - Basilico, Nicoletta
AU  - Gamarro, Francisco
AU  - Šolaja, Bogdan A.
PY  - 2019
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/3288
PB  - Elsevier
T2  - European Journal of Medicinal Chemistry
T1  - Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010
ER  - 
@book{
author = "Manzano, Jose Ignacio and Konstantinović, Jelena and Scaccabarozzi, Diletta and Perea, Ana and Pavić, Aleksandar and Cavicchini, Loredana and Basilico, Nicoletta and Gamarro, Francisco and Šolaja, Bogdan A.",
year = "2019",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/3288",
publisher = "Elsevier",
journal = "European Journal of Medicinal Chemistry",
title = "Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010"
}
Manzano, J. I., Konstantinović, J., Scaccabarozzi, D., Perea, A., Pavić, A., Cavicchini, L., Basilico, N., Gamarro, F.,& Šolaja, B. A. (2019). Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010.
European Journal of Medicinal Chemistry
Elsevier..
Manzano JI, Konstantinović J, Scaccabarozzi D, Perea A, Pavić A, Cavicchini L, Basilico N, Gamarro F, Šolaja BA. Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010. European Journal of Medicinal Chemistry. 2019;
Manzano Jose Ignacio, Konstantinović Jelena, Scaccabarozzi Diletta, Perea Ana, Pavić Aleksandar, Cavicchini Loredana, Basilico Nicoletta, Gamarro Francisco, Šolaja Bogdan A., "Supplementary material for the article: Manzano, J. I.; Konstantinović, J.; Scaccabarozzi, D.; Perea, A.; Pavić, A.; Cavicchini, L.; Basilico, N.; Gamarro, F.; Šolaja, B. A. 4-Aminoquinoline-Based Compounds as Antileishmanial Agents That Inhibit the Energy Metabolism of Leishmania. European Journal of Medicinal Chemistry 2019, 180, 28–40. https://doi.org/10.1016/j.ejmech.2019.07.010" European Journal of Medicinal Chemistry (2019)

Human serum albumin binding of certain antimalarials

Marković, Olivera S.; Cvijetić, Ilija; Zlatović, Mario; Opsenica, Igor; Konstantinović, Jelena M.; Terzić-Jovanović, Nataša; Šolaja, Bogdan A.; Verbić, Tatjana

(Pergamon-Elsevier Science Ltd, Oxford, 2018)

TY  - JOUR
AU  - Marković, Olivera S.
AU  - Cvijetić, Ilija
AU  - Zlatović, Mario
AU  - Opsenica, Igor
AU  - Konstantinović, Jelena M.
AU  - Terzić-Jovanović, Nataša
AU  - Šolaja, Bogdan A.
AU  - Verbić, Tatjana
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2085
AB  - Interactions between eight in-house synthesized aminoquinolines, along with well-known chloroquine, and human serum albumin (HSA) have been studied by fluorescence spectroscopy. The synthesized aminoquinolines, despite being structurally diverse, were found to be very potent antimalarials. Fluorescence measurements indicate that three compounds having additional thiophene or benzothiophene substructure bind more strongly to HSA than other studied compounds. Competitive binding experiments indicate that these three compounds bind significantly stronger to warfarin compared to diazepam binding site. Fluorescence quenching at three temperatures (20, 25, and 37 degrees C) was analyzed using classical Stern-Volmer equation, and a static quenching mechanism was proposed. The enthalpy and entropy changes upon sulphur-containing compound-HSA interactions were calculated using Van't Hoff equation. Positive values of enthalpy and entropy changes indicate that non-specific, hydrophobic interactions are the main contributors to HSA-compound interaction. Molecular docking and calculated lipophilicity descriptors indicate the same, pointing out that the increased lipophilicity of sulphur-containing compounds might be a reason for their better binding to HSA. Obtained results might contribute to design of novel derivatives with improved-pharmacokinetic properties and drug efficacy. (C) 2017 Elsevier B.V. All rights reserved.
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
T1  - Human serum albumin binding of certain antimalarials
VL  - 192
SP  - 128
EP  - 139
DO  - 10.1016/j.saa.2017.10.061
ER  - 
@article{
author = "Marković, Olivera S. and Cvijetić, Ilija and Zlatović, Mario and Opsenica, Igor and Konstantinović, Jelena M. and Terzić-Jovanović, Nataša and Šolaja, Bogdan A. and Verbić, Tatjana",
year = "2018",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2085",
abstract = "Interactions between eight in-house synthesized aminoquinolines, along with well-known chloroquine, and human serum albumin (HSA) have been studied by fluorescence spectroscopy. The synthesized aminoquinolines, despite being structurally diverse, were found to be very potent antimalarials. Fluorescence measurements indicate that three compounds having additional thiophene or benzothiophene substructure bind more strongly to HSA than other studied compounds. Competitive binding experiments indicate that these three compounds bind significantly stronger to warfarin compared to diazepam binding site. Fluorescence quenching at three temperatures (20, 25, and 37 degrees C) was analyzed using classical Stern-Volmer equation, and a static quenching mechanism was proposed. The enthalpy and entropy changes upon sulphur-containing compound-HSA interactions were calculated using Van't Hoff equation. Positive values of enthalpy and entropy changes indicate that non-specific, hydrophobic interactions are the main contributors to HSA-compound interaction. Molecular docking and calculated lipophilicity descriptors indicate the same, pointing out that the increased lipophilicity of sulphur-containing compounds might be a reason for their better binding to HSA. Obtained results might contribute to design of novel derivatives with improved-pharmacokinetic properties and drug efficacy. (C) 2017 Elsevier B.V. All rights reserved.",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy",
title = "Human serum albumin binding of certain antimalarials",
volume = "192",
pages = "128-139",
doi = "10.1016/j.saa.2017.10.061"
}
Marković, O. S., Cvijetić, I., Zlatović, M., Opsenica, I., Konstantinović, J. M., Terzić-Jovanović, N., Šolaja, B. A.,& Verbić, T. (2018). Human serum albumin binding of certain antimalarials.
Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
Pergamon-Elsevier Science Ltd, Oxford., 192, 128-139.
https://doi.org/10.1016/j.saa.2017.10.061
Marković OS, Cvijetić I, Zlatović M, Opsenica I, Konstantinović JM, Terzić-Jovanović N, Šolaja BA, Verbić T. Human serum albumin binding of certain antimalarials. Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy. 2018;192:128-139
Marković Olivera S., Cvijetić Ilija, Zlatović Mario, Opsenica Igor, Konstantinović Jelena M., Terzić-Jovanović Nataša, Šolaja Bogdan A., Verbić Tatjana, "Human serum albumin binding of certain antimalarials" Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy, 192 (2018):128-139,
https://doi.org/10.1016/j.saa.2017.10.061 .
10
10
10

Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061

Marković, Olivera S.; Cvijetić, Ilija; Zlatović, Mario; Opsenica, Igor; Konstantinović, Jelena M.; Terzić-Jovanović, Nataša; Šolaja, Bogdan A.; Verbić, Tatjana

(Pergamon-Elsevier Science Ltd, Oxford, 2018)

TY  - BOOK
AU  - Marković, Olivera S.
AU  - Cvijetić, Ilija
AU  - Zlatović, Mario
AU  - Opsenica, Igor
AU  - Konstantinović, Jelena M.
AU  - Terzić-Jovanović, Nataša
AU  - Šolaja, Bogdan A.
AU  - Verbić, Tatjana
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2913
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
T1  - Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061
ER  - 
@book{
author = "Marković, Olivera S. and Cvijetić, Ilija and Zlatović, Mario and Opsenica, Igor and Konstantinović, Jelena M. and Terzić-Jovanović, Nataša and Šolaja, Bogdan A. and Verbić, Tatjana",
year = "2018",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2913",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy",
title = "Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061"
}
Marković, O. S., Cvijetić, I., Zlatović, M., Opsenica, I., Konstantinović, J. M., Terzić-Jovanović, N., Šolaja, B. A.,& Verbić, T. (2018). Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061.
Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy
Pergamon-Elsevier Science Ltd, Oxford..
Marković OS, Cvijetić I, Zlatović M, Opsenica I, Konstantinović JM, Terzić-Jovanović N, Šolaja BA, Verbić T. Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061. Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy. 2018;
Marković Olivera S., Cvijetić Ilija, Zlatović Mario, Opsenica Igor, Konstantinović Jelena M., Terzić-Jovanović Nataša, Šolaja Bogdan A., Verbić Tatjana, "Supplementary data for the article: Marković, O. S.; Cvijetić, I. N.; Zlatović, M. V.; Opsenica, I. M.; Konstantinović, J. M.; Terzić Jovanović, N. V.; Šolaja, B. A.; Verbić, T. Ž. Human Serum Albumin Binding of Certain Antimalarials. Spectrochimica Acta - Part A: Molecular and Biomolecular Spectroscopy 2018, 192, 128–139. https://doi.org/10.1016/j.saa.2017.10.061" Spectrochimica Acta. Part A: Molecular and Biomolecular Spectroscopy (2018)

Dizajn i sinteza inhibitora botulinum neurotoksina A i parazita Plasmodium falciparum

Konstantinović, Jelena M.

(Универзитет у Београду, Хемијски факултет, 2018)

TY  - BOOK
AU  - Konstantinović, Jelena M.
PY  - 2018
UR  - http://eteze.bg.ac.rs/application/showtheses?thesesId=5940
UR  - https://fedorabg.bg.ac.rs/fedora/get/o:18090/bdef:Content/download
UR  - http://vbs.rs/scripts/cobiss?command=DISPLAY&base=70036&RID=50361871
UR  - http://nardus.mpn.gov.rs/123456789/9791
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2766
AB  - Botulinum neurotoksini su najjaĉi poznati prirodni otrovi i izazivaĉi botulizma –potencijalno smrtonosne neuroparalitiĉke bolesti. U poslednje vreme, sve veći brojstudija je usmeren ka pronalaţenju inhibitora botulinum neurotoksina serotipa A(BoNT/A) aktivnih unutar ćelije, jer terapija antitelima ima uspeha jedino pre nego štotoksin uĊe u neuron. U okviru ove doktorske disertacije izvršena je sinteza i detaljnoispitivanje inhibitorne aktivnosti novih steroidnih i benzo[b]tiofenskih derivata4-aminohinolina prema kratkom nizu (BoNT/A LC) i holotoksinu BoNT/A. Uistraţivanju je korišćen proteolitiĉki in vitro esej i ćelijski esej u motornim neuronimarazvijenim iz embrionalnih matiĉnih ćelija miša (mES-MN). Dodatno, molekulskomodelovanje i uklapanje novih derivata u aktivno mesto enzima izvršeno je korišćenjemprograma Schr dinger Suite 2016-4.U in vitro proteolitiĉkom eseju, sintetisana jedinjenja su ostvarila do 85%inhibicije BoNT/A LC pri koncentraciji 20 μM, dok su IC50 vrednosti bile u opsegu 0,7–10,2 μM. U preintoksikacionom modelu u motornim neuronima razvijenim izembrionalnih matiĉnih ćelija miša (mES-MN) novi derivati su vršili zaštitu proteinaSNAP-25i do 88%, u niskim mikromolarnim koncentracijama i u dozno-zavisnomreţimu. Najaktivniji derivati su testirani u postintoksikacionom modelu, u kome sejedinjenja dodaju ćelijskoj kulturi 30 ili 60 minuta posle holotoksina. U oba modela jeuoĉena korelacija procenta zaštite SNAP-25 i primenjene koncentracije jedinjenja.Jedinjenje 17 (JK141) je pokazalo 99% zaštite SNAP-25 kada se administrira 30 minutaposle BoNT/A...
AB  - Botulinum neurotoxins are the most poisonous (biological) substances knownand causative agents of botulism – serious and potentially fatal neuroparalytic illness.Recently, the majority of efforts have focused on identification of botulinum neurotoxinserotype A (BoNT/A) inhibitors with intracellular activity, because antibody-basedtreatments are successful only before toxin enters a neuron. In this doctoral dissertationsynthesis and detailed evaluation of inhibitory potencies of new steroidal andbenzo[b]thiophene 4-aminoquinoline derivatives against BoNT/A light chain (LC) andfull length BoNT/A is reported. Both in vitro proteolytic assay and cell-based assayusing mouse embryonic stem cell derived motor neurons (mES-MNs) were employed.To rationalize the inhibitory potencies of the new derivatives, structure-based dockingsimulations were performed using Schr dinger Suite 2016-4 and the modules therein.Using in vitro HPLC-based assay, the newly synthesized molecules have shownBoNT/A LC inhibition up to 85% at 20 μM and IC50 values ranging from 0.7–10.2 μM.Compounds tested during BoNT/A challenge in mES-MNs in preintoxication modelwere found to protect SNAP-25 proteinii by up to 88% at low μM concentrations and indose-dependent manner. The most effective derivatives were also tested in a postexposuremodel, where compounds were added 30 or 60 minutes following holotoxinadministration. In both pre- and postintoxication models, dose-dependent behavior wasobserved. Compound 17 (JK141) showed 99% of SNAP-25 cleavage protection whenadministrated 30 minutes after BoNT/A...
PB  - Универзитет у Београду, Хемијски факултет
T2  - Универзитет у Београду
T1  - Dizajn i sinteza inhibitora botulinum neurotoksina A i parazita Plasmodium falciparum
ER  - 
@phdthesis{
author = "Konstantinović, Jelena M.",
year = "2018",
url = "http://eteze.bg.ac.rs/application/showtheses?thesesId=5940, https://fedorabg.bg.ac.rs/fedora/get/o:18090/bdef:Content/download, http://vbs.rs/scripts/cobiss?command=DISPLAY&base=70036&RID=50361871, http://nardus.mpn.gov.rs/123456789/9791, http://cherry.chem.bg.ac.rs/handle/123456789/2766",
abstract = "Botulinum neurotoksini su najjaĉi poznati prirodni otrovi i izazivaĉi botulizma –potencijalno smrtonosne neuroparalitiĉke bolesti. U poslednje vreme, sve veći brojstudija je usmeren ka pronalaţenju inhibitora botulinum neurotoksina serotipa A(BoNT/A) aktivnih unutar ćelije, jer terapija antitelima ima uspeha jedino pre nego štotoksin uĊe u neuron. U okviru ove doktorske disertacije izvršena je sinteza i detaljnoispitivanje inhibitorne aktivnosti novih steroidnih i benzo[b]tiofenskih derivata4-aminohinolina prema kratkom nizu (BoNT/A LC) i holotoksinu BoNT/A. Uistraţivanju je korišćen proteolitiĉki in vitro esej i ćelijski esej u motornim neuronimarazvijenim iz embrionalnih matiĉnih ćelija miša (mES-MN). Dodatno, molekulskomodelovanje i uklapanje novih derivata u aktivno mesto enzima izvršeno je korišćenjemprograma Schr dinger Suite 2016-4.U in vitro proteolitiĉkom eseju, sintetisana jedinjenja su ostvarila do 85%inhibicije BoNT/A LC pri koncentraciji 20 μM, dok su IC50 vrednosti bile u opsegu 0,7–10,2 μM. U preintoksikacionom modelu u motornim neuronima razvijenim izembrionalnih matiĉnih ćelija miša (mES-MN) novi derivati su vršili zaštitu proteinaSNAP-25i do 88%, u niskim mikromolarnim koncentracijama i u dozno-zavisnomreţimu. Najaktivniji derivati su testirani u postintoksikacionom modelu, u kome sejedinjenja dodaju ćelijskoj kulturi 30 ili 60 minuta posle holotoksina. U oba modela jeuoĉena korelacija procenta zaštite SNAP-25 i primenjene koncentracije jedinjenja.Jedinjenje 17 (JK141) je pokazalo 99% zaštite SNAP-25 kada se administrira 30 minutaposle BoNT/A..., Botulinum neurotoxins are the most poisonous (biological) substances knownand causative agents of botulism – serious and potentially fatal neuroparalytic illness.Recently, the majority of efforts have focused on identification of botulinum neurotoxinserotype A (BoNT/A) inhibitors with intracellular activity, because antibody-basedtreatments are successful only before toxin enters a neuron. In this doctoral dissertationsynthesis and detailed evaluation of inhibitory potencies of new steroidal andbenzo[b]thiophene 4-aminoquinoline derivatives against BoNT/A light chain (LC) andfull length BoNT/A is reported. Both in vitro proteolytic assay and cell-based assayusing mouse embryonic stem cell derived motor neurons (mES-MNs) were employed.To rationalize the inhibitory potencies of the new derivatives, structure-based dockingsimulations were performed using Schr dinger Suite 2016-4 and the modules therein.Using in vitro HPLC-based assay, the newly synthesized molecules have shownBoNT/A LC inhibition up to 85% at 20 μM and IC50 values ranging from 0.7–10.2 μM.Compounds tested during BoNT/A challenge in mES-MNs in preintoxication modelwere found to protect SNAP-25 proteinii by up to 88% at low μM concentrations and indose-dependent manner. The most effective derivatives were also tested in a postexposuremodel, where compounds were added 30 or 60 minutes following holotoxinadministration. In both pre- and postintoxication models, dose-dependent behavior wasobserved. Compound 17 (JK141) showed 99% of SNAP-25 cleavage protection whenadministrated 30 minutes after BoNT/A...",
publisher = "Универзитет у Београду, Хемијски факултет",
journal = "Универзитет у Београду",
title = "Dizajn i sinteza inhibitora botulinum neurotoksina A i parazita Plasmodium falciparum"
}
Konstantinović, J. M. (2018). Dizajn i sinteza inhibitora botulinum neurotoksina A i parazita Plasmodium falciparum.
Универзитет у Београду
Универзитет у Београду, Хемијски факултет..
Konstantinović JM. Dizajn i sinteza inhibitora botulinum neurotoksina A i parazita Plasmodium falciparum. Универзитет у Београду. 2018;
Konstantinović Jelena M., "Dizajn i sinteza inhibitora botulinum neurotoksina A i parazita Plasmodium falciparum" Универзитет у Београду (2018)

Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice

Konstantinović, Jelena M.; Selaković, Milica; Orsini, Stefania; Bogojević, Katarina; D'Alessandro, Sarah; Scaccabarozzi, Diletta; Terzić-Jovanović, Nataša; Gradoni, Luigi; Basilico, Nicoletta; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2018)

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Selaković, Milica
AU  - Orsini, Stefania
AU  - Bogojević, Katarina
AU  - D'Alessandro, Sarah
AU  - Scaccabarozzi, Diletta
AU  - Terzić-Jovanović, Nataša
AU  - Gradoni, Luigi
AU  - Basilico, Nicoletta
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2948
AB  - In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.
PB  - Amer Chemical Soc, Washington
T2  - ACS Medicinal Chemistry Letters
T1  - Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
VL  - 9
IS  - 7
SP  - 629
EP  - 634
DO  - 10.1021/acsmedchemlett.8b00053
ER  - 
@article{
author = "Konstantinović, Jelena M. and Selaković, Milica and Orsini, Stefania and Bogojević, Katarina and D'Alessandro, Sarah and Scaccabarozzi, Diletta and Terzić-Jovanović, Nataša and Gradoni, Luigi and Basilico, Nicoletta and Šolaja, Bogdan A.",
year = "2018",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2948",
abstract = "In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.",
publisher = "Amer Chemical Soc, Washington",
journal = "ACS Medicinal Chemistry Letters",
title = "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice",
volume = "9",
number = "7",
pages = "629-634",
doi = "10.1021/acsmedchemlett.8b00053"
}
Konstantinović, J. M., Selaković, M., Orsini, S., Bogojević, K., D'Alessandro, S., Scaccabarozzi, D., Terzić-Jovanović, N., Gradoni, L., Basilico, N.,& Šolaja, B. A. (2018). Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice.
ACS Medicinal Chemistry Letters
Amer Chemical Soc, Washington., 9(7), 629-634.
https://doi.org/10.1021/acsmedchemlett.8b00053
Konstantinović JM, Selaković M, Orsini S, Bogojević K, D'Alessandro S, Scaccabarozzi D, Terzić-Jovanović N, Gradoni L, Basilico N, Šolaja BA. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. ACS Medicinal Chemistry Letters. 2018;9(7):629-634
Konstantinović Jelena M., Selaković Milica, Orsini Stefania, Bogojević Katarina, D'Alessandro Sarah, Scaccabarozzi Diletta, Terzić-Jovanović Nataša, Gradoni Luigi, Basilico Nicoletta, Šolaja Bogdan A., "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice" ACS Medicinal Chemistry Letters, 9, no. 7 (2018):629-634,
https://doi.org/10.1021/acsmedchemlett.8b00053 .
1
7
5
7

Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053

Konstantinović, Jelena M.; Selaković, Milica; Orsini, Stefania; Bogojević, Katarina; D'Alessandro, Sarah; Scaccabarozzi, Diletta; Terzić-Jovanović, Nataša; Gradoni, Luigi; Basilico, Nicoletta; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2018)

TY  - BOOK
AU  - Konstantinović, Jelena M.
AU  - Selaković, Milica
AU  - Orsini, Stefania
AU  - Bogojević, Katarina
AU  - D'Alessandro, Sarah
AU  - Scaccabarozzi, Diletta
AU  - Terzić-Jovanović, Nataša
AU  - Gradoni, Luigi
AU  - Basilico, Nicoletta
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2949
PB  - Amer Chemical Soc, Washington
T2  - ACS Medicinal Chemistry Letters
T1  - Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053
ER  - 
@book{
author = "Konstantinović, Jelena M. and Selaković, Milica and Orsini, Stefania and Bogojević, Katarina and D'Alessandro, Sarah and Scaccabarozzi, Diletta and Terzić-Jovanović, Nataša and Gradoni, Luigi and Basilico, Nicoletta and Šolaja, Bogdan A.",
year = "2018",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2949",
publisher = "Amer Chemical Soc, Washington",
journal = "ACS Medicinal Chemistry Letters",
title = "Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053"
}
Konstantinović, J. M., Selaković, M., Orsini, S., Bogojević, K., D'Alessandro, S., Scaccabarozzi, D., Terzić-Jovanović, N., Gradoni, L., Basilico, N.,& Šolaja, B. A. (2018). Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053.
ACS Medicinal Chemistry Letters
Amer Chemical Soc, Washington..
Konstantinović JM, Selaković M, Orsini S, Bogojević K, D'Alessandro S, Scaccabarozzi D, Terzić-Jovanović N, Gradoni L, Basilico N, Šolaja BA. Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053. ACS Medicinal Chemistry Letters. 2018;
Konstantinović Jelena M., Selaković Milica, Orsini Stefania, Bogojević Katarina, D'Alessandro Sarah, Scaccabarozzi Diletta, Terzić-Jovanović Nataša, Gradoni Luigi, Basilico Nicoletta, Šolaja Bogdan A., "Supplementary data for the article: Konstantinović, J.; Videnović, M.; Orsini, S.; Bogojević, K.; D’Alessandro, S.; Scaccabarozzi, D.; Terzić Jovanović, N.; Gradoni, L.; Basilico, N.; Šolaja, B. A. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania Infantum Infected Mice. ACS Medicinal Chemistry Letters 2018, 9 (7), 629–634. https://doi.org/10.1021/acsmedchemlett.8b00053" ACS Medicinal Chemistry Letters (2018)

Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710

Konstantinović, Jelena M.; Kiris, Erkan; Kota, Krishna P.; Kugelman-Tonos, Johanny; Selaković, Milica; Cazares, Lisa H.; Terzić-Jovanović, Nataša; Verbić, Tatjana; Anđelković, Boban D.; Duplantier, Allen J.; Bavari, Sina; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2018)

TY  - BOOK
AU  - Konstantinović, Jelena M.
AU  - Kiris, Erkan
AU  - Kota, Krishna P.
AU  - Kugelman-Tonos, Johanny
AU  - Selaković, Milica
AU  - Cazares, Lisa H.
AU  - Terzić-Jovanović, Nataša
AU  - Verbić, Tatjana
AU  - Anđelković, Boban D.
AU  - Duplantier, Allen J.
AU  - Bavari, Sina
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/3039
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710
ER  - 
@book{
author = "Konstantinović, Jelena M. and Kiris, Erkan and Kota, Krishna P. and Kugelman-Tonos, Johanny and Selaković, Milica and Cazares, Lisa H. and Terzić-Jovanović, Nataša and Verbić, Tatjana and Anđelković, Boban D. and Duplantier, Allen J. and Bavari, Sina and Šolaja, Bogdan A.",
year = "2018",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/3039",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710"
}
Konstantinović, J. M., Kiris, E., Kota, K. P., Kugelman-Tonos, J., Selaković, M., Cazares, L. H., Terzić-Jovanović, N., Verbić, T., Anđelković, B. D., Duplantier, A. J., Bavari, S.,& Šolaja, B. A. (2018). Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710.
Journal of Medicinal Chemistry
Amer Chemical Soc, Washington..
Konstantinović JM, Kiris E, Kota KP, Kugelman-Tonos J, Selaković M, Cazares LH, Terzić-Jovanović N, Verbić T, Anđelković BD, Duplantier AJ, Bavari S, Šolaja BA. Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710. Journal of Medicinal Chemistry. 2018;
Konstantinović Jelena M., Kiris Erkan, Kota Krishna P., Kugelman-Tonos Johanny, Selaković Milica, Cazares Lisa H., Terzić-Jovanović Nataša, Verbić Tatjana, Anđelković Boban D., Duplantier Allen J., Bavari Sina, Šolaja Bogdan A., "Supplementary data for the article: Konstantinović, J.; Kiris, E.; Kota, K. P.; Kugelman-Tonos, J.; Videnović, M.; Cazares, L. H.; Terzić Jovanović, N.; Verbić, T. Ž.; Andjelković, B.; Duplantier, A. J.; et al. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry 2018, 61 (4), 1595–1608. https://doi.org/10.1021/acs.jmedchem.7b01710" Journal of Medicinal Chemistry (2018)

New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model

Konstantinović, Jelena M.; Kiris, Erkan; Kota, Krishna P.; Kugelman-Tonos, Johanny; Selaković, Milica; Cazares, Lisa H.; Terzić-Jovanović, Nataša; Verbić, Tatjana; Anđelković, Boban D.; Duplantier, Allen J.; Bavari, Sina; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2018)

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Kiris, Erkan
AU  - Kota, Krishna P.
AU  - Kugelman-Tonos, Johanny
AU  - Selaković, Milica
AU  - Cazares, Lisa H.
AU  - Terzić-Jovanović, Nataša
AU  - Verbić, Tatjana
AU  - Anđelković, Boban D.
AU  - Duplantier, Allen J.
AU  - Bavari, Sina
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2099
AB  - The synthesis and inhibitory potencies against botulinum neurotoxin serotype A light chain (BoNT/A LC) using in vitro HPLC based enzymatic assay for various steroidal, benzothiophene, thiophene, and adamantane 4-aminoquinoline derivatives are described. In addition, the compounds were evaluated for the activity against BoNT/A holotoxin in mouse embryonic stem cell derived motor neurons. Steroidal derivative 16 showed remarkable protection (up to 89% of uncleaved SNAP-25) even when administered 30 min postintoxication. This appears to be the first example of LC inhibitors antagonizing BoNT intoxication in mouse embryonic stem cell derived motor neurons (mES-MNs) in a postexposure model. Oral administration of 16 was well tolerated in the mouse up to 600 mg/kg, q.d. Although adequate unbound drug levels were not achieved at this dose, the favorable in vitro ADMET results strongly support further work in this series.
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model
VL  - 61
IS  - 4
SP  - 1595
EP  - 1608
DO  - 10.1021/acs.jmedchem.7b01710
ER  - 
@article{
author = "Konstantinović, Jelena M. and Kiris, Erkan and Kota, Krishna P. and Kugelman-Tonos, Johanny and Selaković, Milica and Cazares, Lisa H. and Terzić-Jovanović, Nataša and Verbić, Tatjana and Anđelković, Boban D. and Duplantier, Allen J. and Bavari, Sina and Šolaja, Bogdan A.",
year = "2018",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2099",
abstract = "The synthesis and inhibitory potencies against botulinum neurotoxin serotype A light chain (BoNT/A LC) using in vitro HPLC based enzymatic assay for various steroidal, benzothiophene, thiophene, and adamantane 4-aminoquinoline derivatives are described. In addition, the compounds were evaluated for the activity against BoNT/A holotoxin in mouse embryonic stem cell derived motor neurons. Steroidal derivative 16 showed remarkable protection (up to 89% of uncleaved SNAP-25) even when administered 30 min postintoxication. This appears to be the first example of LC inhibitors antagonizing BoNT intoxication in mouse embryonic stem cell derived motor neurons (mES-MNs) in a postexposure model. Oral administration of 16 was well tolerated in the mouse up to 600 mg/kg, q.d. Although adequate unbound drug levels were not achieved at this dose, the favorable in vitro ADMET results strongly support further work in this series.",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model",
volume = "61",
number = "4",
pages = "1595-1608",
doi = "10.1021/acs.jmedchem.7b01710"
}
Konstantinović, J. M., Kiris, E., Kota, K. P., Kugelman-Tonos, J., Selaković, M., Cazares, L. H., Terzić-Jovanović, N., Verbić, T., Anđelković, B. D., Duplantier, A. J., Bavari, S.,& Šolaja, B. A. (2018). New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model.
Journal of Medicinal Chemistry
Amer Chemical Soc, Washington., 61(4), 1595-1608.
https://doi.org/10.1021/acs.jmedchem.7b01710
Konstantinović JM, Kiris E, Kota KP, Kugelman-Tonos J, Selaković M, Cazares LH, Terzić-Jovanović N, Verbić T, Anđelković BD, Duplantier AJ, Bavari S, Šolaja BA. New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model. Journal of Medicinal Chemistry. 2018;61(4):1595-1608
Konstantinović Jelena M., Kiris Erkan, Kota Krishna P., Kugelman-Tonos Johanny, Selaković Milica, Cazares Lisa H., Terzić-Jovanović Nataša, Verbić Tatjana, Anđelković Boban D., Duplantier Allen J., Bavari Sina, Šolaja Bogdan A., "New Steroidal 4-Aminoquinolines Antagonize Botulinum Neurotoxin Serotype A in Mouse Embryonic Stem Cell Derived Motor Neurons in Postintoxication Model" Journal of Medicinal Chemistry, 61, no. 4 (2018):1595-1608,
https://doi.org/10.1021/acs.jmedchem.7b01710 .
3
3
3

Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice

Konstantinović, Jelena M.; Selaković, Milica; Orsini, Stefania; Bogojević, Katarina; D'Alessandro, Sarah; Scaccabarozzi, Diletta; Terzić-Jovanović, Nataša; Gradoni, Luigi; Basilico, Nicoletta; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2018)

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Selaković, Milica
AU  - Orsini, Stefania
AU  - Bogojević, Katarina
AU  - D'Alessandro, Sarah
AU  - Scaccabarozzi, Diletta
AU  - Terzić-Jovanović, Nataša
AU  - Gradoni, Luigi
AU  - Basilico, Nicoletta
AU  - Šolaja, Bogdan A.
PY  - 2018
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2209
AB  - In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.
PB  - Amer Chemical Soc, Washington
T2  - ACS Medicinal Chemistry Letters
T1  - Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
VL  - 9
IS  - 7
SP  - 629
EP  - 634
DO  - 10.1021/acsmedchemlett.8b00053
ER  - 
@article{
author = "Konstantinović, Jelena M. and Selaković, Milica and Orsini, Stefania and Bogojević, Katarina and D'Alessandro, Sarah and Scaccabarozzi, Diletta and Terzić-Jovanović, Nataša and Gradoni, Luigi and Basilico, Nicoletta and Šolaja, Bogdan A.",
year = "2018",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2209",
abstract = "In this Letter, a detailed analysis of 30 4-aminoquinoline-based compounds with regard to their potential as antileishmanial drugs has been carried out. Ten compounds demonstrated IC50  lt  1 mu M against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50  lt  1 mu M against intramacrophage L. infantum amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarkable reduction of parasite load in vivo, with advantage of being short-term and orally active. To the best of our knowledge, this is the first example of 4-amino-7-chloroquinoline derivatives active in Leishmania infantum infected mice.",
publisher = "Amer Chemical Soc, Washington",
journal = "ACS Medicinal Chemistry Letters",
title = "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice",
volume = "9",
number = "7",
pages = "629-634",
doi = "10.1021/acsmedchemlett.8b00053"
}
Konstantinović, J. M., Selaković, M., Orsini, S., Bogojević, K., D'Alessandro, S., Scaccabarozzi, D., Terzić-Jovanović, N., Gradoni, L., Basilico, N.,& Šolaja, B. A. (2018). Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice.
ACS Medicinal Chemistry Letters
Amer Chemical Soc, Washington., 9(7), 629-634.
https://doi.org/10.1021/acsmedchemlett.8b00053
Konstantinović JM, Selaković M, Orsini S, Bogojević K, D'Alessandro S, Scaccabarozzi D, Terzić-Jovanović N, Gradoni L, Basilico N, Šolaja BA. Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice. ACS Medicinal Chemistry Letters. 2018;9(7):629-634
Konstantinović Jelena M., Selaković Milica, Orsini Stefania, Bogojević Katarina, D'Alessandro Sarah, Scaccabarozzi Diletta, Terzić-Jovanović Nataša, Gradoni Luigi, Basilico Nicoletta, Šolaja Bogdan A., "Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice" ACS Medicinal Chemistry Letters, 9, no. 7 (2018):629-634,
https://doi.org/10.1021/acsmedchemlett.8b00053 .
1
7
5
7

Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners

Konstantinović, Jelena M.; Selaković, Milica; Srbljanović, Jelena; Đurković-Đaković, Olgica; Bogojević, Katarina; Sciotti, Richard; Šolaja, Bogdan A.

(Mdpi Ag, Basel, 2017)

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Selaković, Milica
AU  - Srbljanović, Jelena
AU  - Đurković-Đaković, Olgica
AU  - Bogojević, Katarina
AU  - Sciotti, Richard
AU  - Šolaja, Bogdan A.
PY  - 2017
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2441
AB  - Malaria is a severe and life-threatening disease caused by Plasmodium parasites that are spread to humans through bites of infected Anopheles mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting Plasmodium falciparum parasite growth. Synthesized compounds were evaluated for their antimalarial activity and toxicity, in vitro and in mice. Benzothiophenes presented in this paper showed improved activities against a chloroquine susceptible (CQS) strain, with potencies of IC50 = 6 nM, and cured 5/5 Plasmodium berghei infected mice when dosed orally at 160 mg/kg/day x 3 days. In the benzothiophene series, the examined antiplasmodials were more active against the CQS strain D6, than against strains chloroquine resistant (CQR) W2 and multidrug-resistant (MDR) TM91C235. For the thiophene series, a very interesting feature was revealed: hypersensitivity to the CQR strains, resistance index (RI) of  lt  1. This is in sharp contrast to chloroquine, indicating that further development of the series would provide us with more potent antimalarials against CQR strains.
PB  - Mdpi Ag, Basel
T2  - Molecules
T1  - Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners
VL  - 22
IS  - 3
DO  - 10.3390/molecules22030343
ER  - 
@article{
author = "Konstantinović, Jelena M. and Selaković, Milica and Srbljanović, Jelena and Đurković-Đaković, Olgica and Bogojević, Katarina and Sciotti, Richard and Šolaja, Bogdan A.",
year = "2017",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2441",
abstract = "Malaria is a severe and life-threatening disease caused by Plasmodium parasites that are spread to humans through bites of infected Anopheles mosquitoes. Here, we report on the efficacy of aminoquinolines coupled to benzothiophene and thiophene rings in inhibiting Plasmodium falciparum parasite growth. Synthesized compounds were evaluated for their antimalarial activity and toxicity, in vitro and in mice. Benzothiophenes presented in this paper showed improved activities against a chloroquine susceptible (CQS) strain, with potencies of IC50 = 6 nM, and cured 5/5 Plasmodium berghei infected mice when dosed orally at 160 mg/kg/day x 3 days. In the benzothiophene series, the examined antiplasmodials were more active against the CQS strain D6, than against strains chloroquine resistant (CQR) W2 and multidrug-resistant (MDR) TM91C235. For the thiophene series, a very interesting feature was revealed: hypersensitivity to the CQR strains, resistance index (RI) of  lt  1. This is in sharp contrast to chloroquine, indicating that further development of the series would provide us with more potent antimalarials against CQR strains.",
publisher = "Mdpi Ag, Basel",
journal = "Molecules",
title = "Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners",
volume = "22",
number = "3",
doi = "10.3390/molecules22030343"
}
Konstantinović, J. M., Selaković, M., Srbljanović, J., Đurković-Đaković, O., Bogojević, K., Sciotti, R.,& Šolaja, B. A. (2017). Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners.
Molecules
Mdpi Ag, Basel., 22(3).
https://doi.org/10.3390/molecules22030343
Konstantinović JM, Selaković M, Srbljanović J, Đurković-Đaković O, Bogojević K, Sciotti R, Šolaja BA. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules. 2017;22(3)
Konstantinović Jelena M., Selaković Milica, Srbljanović Jelena, Đurković-Đaković Olgica, Bogojević Katarina, Sciotti Richard, Šolaja Bogdan A., "Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners" Molecules, 22, no. 3 (2017),
https://doi.org/10.3390/molecules22030343 .
1
11
9
12

Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy

Srbljanović, Jelena; Štajner, Tijana; Konstantinović, Jelena M.; Terzić-Jovanović, Nataša; Uzelac, Aleksandra; Bobić, Branko; Šolaja, Bogdan A.; Đurković-Đaković, Olgica

(Elsevier Science Bv, Amsterdam, 2017)

TY  - JOUR
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Konstantinović, Jelena M.
AU  - Terzić-Jovanović, Nataša
AU  - Uzelac, Aleksandra
AU  - Bobić, Branko
AU  - Šolaja, Bogdan A.
AU  - Đurković-Đaković, Olgica
PY  - 2017
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2514
AB  - Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of  gt = 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded  gt = 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines.
PB  - Elsevier Science Bv, Amsterdam
T2  - International Journal of Antimicrobial Agents
T1  - Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy
VL  - 50
IS  - 3
SP  - 461
EP  - 466
DO  - 10.1016/j.ijantimicag.2017.06.002
ER  - 
@article{
author = "Srbljanović, Jelena and Štajner, Tijana and Konstantinović, Jelena M. and Terzić-Jovanović, Nataša and Uzelac, Aleksandra and Bobić, Branko and Šolaja, Bogdan A. and Đurković-Đaković, Olgica",
year = "2017",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2514",
abstract = "Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of  gt = 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded  gt = 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines.",
publisher = "Elsevier Science Bv, Amsterdam",
journal = "International Journal of Antimicrobial Agents",
title = "Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy",
volume = "50",
number = "3",
pages = "461-466",
doi = "10.1016/j.ijantimicag.2017.06.002"
}
Srbljanović, J., Štajner, T., Konstantinović, J. M., Terzić-Jovanović, N., Uzelac, A., Bobić, B., Šolaja, B. A.,& Đurković-Đaković, O. (2017). Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy.
International Journal of Antimicrobial Agents
Elsevier Science Bv, Amsterdam., 50(3), 461-466.
https://doi.org/10.1016/j.ijantimicag.2017.06.002
Srbljanović J, Štajner T, Konstantinović JM, Terzić-Jovanović N, Uzelac A, Bobić B, Šolaja BA, Đurković-Đaković O. Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy. International Journal of Antimicrobial Agents. 2017;50(3):461-466
Srbljanović Jelena, Štajner Tijana, Konstantinović Jelena M., Terzić-Jovanović Nataša, Uzelac Aleksandra, Bobić Branko, Šolaja Bogdan A., Đurković-Đaković Olgica, "Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy" International Journal of Antimicrobial Agents, 50, no. 3 (2017):461-466,
https://doi.org/10.1016/j.ijantimicag.2017.06.002 .
1
2
2
3

Supplementary data for article : Konstantinović, J. M.; Selaković, M.; Srbljanovic, J.; Djurkovic-Djakovic, O.; Bogojević, K.; Sciotti, R.; Šolaja, B. A. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules 2017, 22 (3). https://doi.org/10.3390/molecules22030343

Konstantinović, Jelena M.; Selaković, Milica; Srbljanović, Jelena; Đurković-Đaković, Olgica; Bogojević, Katarina; Sciotti, Richard; Šolaja, Bogdan A.

(Mdpi Ag, Basel, 2017)

TY  - BOOK
AU  - Konstantinović, Jelena M.
AU  - Selaković, Milica
AU  - Srbljanović, Jelena
AU  - Đurković-Đaković, Olgica
AU  - Bogojević, Katarina
AU  - Sciotti, Richard
AU  - Šolaja, Bogdan A.
PY  - 2017
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/3022
PB  - Mdpi Ag, Basel
T2  - Molecules
T1  - Supplementary data for article : Konstantinović, J. M.; Selaković, M.; Srbljanovic, J.; Djurkovic-Djakovic, O.; Bogojević, K.; Sciotti, R.; Šolaja, B. A. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules 2017, 22 (3). https://doi.org/10.3390/molecules22030343
ER  - 
@book{
author = "Konstantinović, Jelena M. and Selaković, Milica and Srbljanović, Jelena and Đurković-Đaković, Olgica and Bogojević, Katarina and Sciotti, Richard and Šolaja, Bogdan A.",
year = "2017",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/3022",
publisher = "Mdpi Ag, Basel",
journal = "Molecules",
title = "Supplementary data for article : Konstantinović, J. M.; Selaković, M.; Srbljanovic, J.; Djurkovic-Djakovic, O.; Bogojević, K.; Sciotti, R.; Šolaja, B. A. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules 2017, 22 (3). https://doi.org/10.3390/molecules22030343"
}
Konstantinović, J. M., Selaković, M., Srbljanović, J., Đurković-Đaković, O., Bogojević, K., Sciotti, R.,& Šolaja, B. A. (2017). Supplementary data for article : Konstantinović, J. M.; Selaković, M.; Srbljanovic, J.; Djurkovic-Djakovic, O.; Bogojević, K.; Sciotti, R.; Šolaja, B. A. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules 2017, 22 (3). https://doi.org/10.3390/molecules22030343.
Molecules
Mdpi Ag, Basel..
Konstantinović JM, Selaković M, Srbljanović J, Đurković-Đaković O, Bogojević K, Sciotti R, Šolaja BA. Supplementary data for article : Konstantinović, J. M.; Selaković, M.; Srbljanovic, J.; Djurkovic-Djakovic, O.; Bogojević, K.; Sciotti, R.; Šolaja, B. A. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules 2017, 22 (3). https://doi.org/10.3390/molecules22030343. Molecules. 2017;
Konstantinović Jelena M., Selaković Milica, Srbljanović Jelena, Đurković-Đaković Olgica, Bogojević Katarina, Sciotti Richard, Šolaja Bogdan A., "Supplementary data for article : Konstantinović, J. M.; Selaković, M.; Srbljanovic, J.; Djurkovic-Djakovic, O.; Bogojević, K.; Sciotti, R.; Šolaja, B. A. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. Molecules 2017, 22 (3). https://doi.org/10.3390/molecules22030343" Molecules (2017)

Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy

Srbljanović, Jelena; Štajner, Tijana; Konstantinović, Jelena M.; Terzić-Jovanović, Nataša; Uzelac, Aleksandra; Bobić, Branko; Šolaja, Bogdan A.; Đurković-Đaković, Olgica

(Elsevier Science Bv, Amsterdam, 2017)

TY  - JOUR
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Konstantinović, Jelena M.
AU  - Terzić-Jovanović, Nataša
AU  - Uzelac, Aleksandra
AU  - Bobić, Branko
AU  - Šolaja, Bogdan A.
AU  - Đurković-Đaković, Olgica
PY  - 2017
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/3214
AB  - Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of  gt = 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded  gt = 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines.
PB  - Elsevier Science Bv, Amsterdam
T2  - International Journal of Antimicrobial Agents
T1  - Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy
VL  - 50
IS  - 3
SP  - 461
EP  - 466
DO  - 10.1016/j.ijantimicag.2017.06.002
ER  - 
@article{
author = "Srbljanović, Jelena and Štajner, Tijana and Konstantinović, Jelena M. and Terzić-Jovanović, Nataša and Uzelac, Aleksandra and Bobić, Branko and Šolaja, Bogdan A. and Đurković-Đaković, Olgica",
year = "2017",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/3214",
abstract = "Malaria remains a major disease in the developing world and globally is the most important parasitic disease causing significant morbidity and mortality. Because of widespread resistance to conventional antimalarials, including chloroquine (CQ), new drugs are urgently needed. Here we report on the antimalarial efficacy, both in vitro and in vivo, of a series of aminoquinoline derivatives with adamantane or benzothiophene as a carrier. In vitro efficacy was evaluated by a lactate dehydrogenase (LDH) assay in cultures of a CQ-sensitive (3D7) and CQ-resistant (Dd2) strain of Plasmodium falcipanim. Of a series of 26 screened compounds, 12 that exerted a growth inhibition rate of  gt = 5% were further examined in vitro to determine the 50% inhibitory concentration (IC50) values. Nine compounds shown in preliminary experiments to be non-toxic in vivo were evaluated in C57BL/6 mice infected with Plasmodium herghei ANKA strain using a modified Thompson test. All nine compounds examined in vivo prolonged the survival of treated versus untreated mice, four of which afforded  gt = 60% survival. Most notably, two of these compounds, both with the adamantane carrier, afforded complete cure (100% survival and parasite clearance). Interestingly, one of these compounds had no in vitro effect against the CQ resistant P. falciparum strain. Better in vivo compared with in vitro results suggest a role for compound metabolites rather than the compounds themselves. The results presented here point to adamantane as a carrier that enhances the antimalarial potential of aminoquinolines.",
publisher = "Elsevier Science Bv, Amsterdam",
journal = "International Journal of Antimicrobial Agents",
title = "Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy",
volume = "50",
number = "3",
pages = "461-466",
doi = "10.1016/j.ijantimicag.2017.06.002"
}
Srbljanović, J., Štajner, T., Konstantinović, J. M., Terzić-Jovanović, N., Uzelac, A., Bobić, B., Šolaja, B. A.,& Đurković-Đaković, O. (2017). Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy.
International Journal of Antimicrobial Agents
Elsevier Science Bv, Amsterdam., 50(3), 461-466.
https://doi.org/10.1016/j.ijantimicag.2017.06.002
Srbljanović J, Štajner T, Konstantinović JM, Terzić-Jovanović N, Uzelac A, Bobić B, Šolaja BA, Đurković-Đaković O. Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy. International Journal of Antimicrobial Agents. 2017;50(3):461-466
Srbljanović Jelena, Štajner Tijana, Konstantinović Jelena M., Terzić-Jovanović Nataša, Uzelac Aleksandra, Bobić Branko, Šolaja Bogdan A., Đurković-Đaković Olgica, "Examination of the antimalarial potential of experimental aminoquinolines: poor in vitro effect does not preclude in vivo efficacy" International Journal of Antimicrobial Agents, 50, no. 3 (2017):461-466,
https://doi.org/10.1016/j.ijantimicag.2017.06.002 .
1
2
2
3

Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?

Terzić-Jovanović, Nataša; Konstantinović, Jelena M.; Tot, Mikloš; Burojević, Jovana; Đurković-Đaković, Olgica; Srbljanović, Jelena; Štajner, Tijana; Verbić, Tatjana; Zlatović, Mario; Machado, Marta; Albuquerque, Ines S.; Prudencio, Miguel; Sciotii, Richard J.; Pečić, Stevan; D'Alessandro, Sarah; Taramelli, Donatella; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2016)

TY  - JOUR
AU  - Terzić-Jovanović, Nataša
AU  - Konstantinović, Jelena M.
AU  - Tot, Mikloš
AU  - Burojević, Jovana
AU  - Đurković-Đaković, Olgica
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Verbić, Tatjana
AU  - Zlatović, Mario
AU  - Machado, Marta
AU  - Albuquerque, Ines S.
AU  - Prudencio, Miguel
AU  - Sciotii, Richard J.
AU  - Pečić, Stevan
AU  - D'Alessandro, Sarah
AU  - Taramelli, Donatella
AU  - Šolaja, Bogdan A.
PY  - 2016
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/2036
AB  - The syntheses and antiplasmodial activities of various substituted aminoquinolines coupled to an adamantane carrier are described. The compounds exhibited pronounced in vitro and in vivo activity against Plasmodium berghei in the Thompson test. Tethering a fluorine atom to the aminoquinoline C(3) position afforded fluoroaminoquinolines that act as intrahepatocytic parasite inhibitors, with compound 25 having an IC50 = 0.31 mu M and reducing the liver load in mice by up to 92% at 80 mg/kg dose. Screening our peroxides as inhibitors of liver stage infection revealed that the tetraoxane pharmacophore itself is also an excellent liver stage P. berghei inhibitor (78: IC50 = 0.33 mu M). Up to 91% reduction of the parasite liver load in mice was achieved at 100 mg/kg. Examination of tetraoxane 78 against the transgenic 3D7 strain expressing luciferase under a gametocyte-specific promoter revealed its activity against stage IV-V Plasmodium falciparum gametocytes (IC50 = 1.16 +/- 0.37 mu M). To the best of our knowledge, compounds 25 and 78 are the first examples of either an 4-aminoquinoline or a tetraoxane liver stage inhibitors.
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?
VL  - 59
IS  - 1
SP  - 264
EP  - 281
DO  - 10.1021/acs.jmedchem.5b01374
ER  - 
@article{
author = "Terzić-Jovanović, Nataša and Konstantinović, Jelena M. and Tot, Mikloš and Burojević, Jovana and Đurković-Đaković, Olgica and Srbljanović, Jelena and Štajner, Tijana and Verbić, Tatjana and Zlatović, Mario and Machado, Marta and Albuquerque, Ines S. and Prudencio, Miguel and Sciotii, Richard J. and Pečić, Stevan and D'Alessandro, Sarah and Taramelli, Donatella and Šolaja, Bogdan A.",
year = "2016",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/2036",
abstract = "The syntheses and antiplasmodial activities of various substituted aminoquinolines coupled to an adamantane carrier are described. The compounds exhibited pronounced in vitro and in vivo activity against Plasmodium berghei in the Thompson test. Tethering a fluorine atom to the aminoquinoline C(3) position afforded fluoroaminoquinolines that act as intrahepatocytic parasite inhibitors, with compound 25 having an IC50 = 0.31 mu M and reducing the liver load in mice by up to 92% at 80 mg/kg dose. Screening our peroxides as inhibitors of liver stage infection revealed that the tetraoxane pharmacophore itself is also an excellent liver stage P. berghei inhibitor (78: IC50 = 0.33 mu M). Up to 91% reduction of the parasite liver load in mice was achieved at 100 mg/kg. Examination of tetraoxane 78 against the transgenic 3D7 strain expressing luciferase under a gametocyte-specific promoter revealed its activity against stage IV-V Plasmodium falciparum gametocytes (IC50 = 1.16 +/- 0.37 mu M). To the best of our knowledge, compounds 25 and 78 are the first examples of either an 4-aminoquinoline or a tetraoxane liver stage inhibitors.",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?",
volume = "59",
number = "1",
pages = "264-281",
doi = "10.1021/acs.jmedchem.5b01374"
}
Terzić-Jovanović, N., Konstantinović, J. M., Tot, M., Burojević, J., Đurković-Đaković, O., Srbljanović, J., Štajner, T., Verbić, T., Zlatović, M., Machado, M., Albuquerque, I. S., Prudencio, M., Sciotii, R. J., Pečić, S., D'Alessandro, S., Taramelli, D.,& Šolaja, B. A. (2016). Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?.
Journal of Medicinal Chemistry
Amer Chemical Soc, Washington., 59(1), 264-281.
https://doi.org/10.1021/acs.jmedchem.5b01374
Terzić-Jovanović N, Konstantinović JM, Tot M, Burojević J, Đurković-Đaković O, Srbljanović J, Štajner T, Verbić T, Zlatović M, Machado M, Albuquerque IS, Prudencio M, Sciotii RJ, Pečić S, D'Alessandro S, Taramelli D, Šolaja BA. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?. Journal of Medicinal Chemistry. 2016;59(1):264-281
Terzić-Jovanović Nataša, Konstantinović Jelena M., Tot Mikloš, Burojević Jovana, Đurković-Đaković Olgica, Srbljanović Jelena, Štajner Tijana, Verbić Tatjana, Zlatović Mario, Machado Marta, Albuquerque Ines S., Prudencio Miguel, Sciotii Richard J., Pečić Stevan, D'Alessandro Sarah, Taramelli Donatella, Šolaja Bogdan A., "Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?" Journal of Medicinal Chemistry, 59, no. 1 (2016):264-281,
https://doi.org/10.1021/acs.jmedchem.5b01374 .
1
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Supplementary data for the article: Terzić, N.; Konstantinović, J.; Tot, M.; Burojević, J.; Djurković-Djaković, O.; Srbljanović, J.; Štajner, T.; Verbić, T.; Zlatović, M.; Machado, M.; et al. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? Journal of Medicinal Chemistry 2016, 59 (1), 264–281. https://doi.org/10.1021/acs.jmedchem.5b01374

Terzić-Jovanović, Nataša; Konstantinović, Jelena M.; Tot, Mikloš; Burojević, Jovana; Đurković-Đaković, Olgica; Srbljanović, Jelena; Štajner, Tijana; Verbić, Tatjana; Zlatović, Mario; Machado, Marta; Albuquerque, Ines S.; Prudencio, Miguel; Sciotii, Richard J.; Pečić, Stevan; D'Alessandro, Sarah; Taramelli, Donatella; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2016)

TY  - BOOK
AU  - Terzić-Jovanović, Nataša
AU  - Konstantinović, Jelena M.
AU  - Tot, Mikloš
AU  - Burojević, Jovana
AU  - Đurković-Đaković, Olgica
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Verbić, Tatjana
AU  - Zlatović, Mario
AU  - Machado, Marta
AU  - Albuquerque, Ines S.
AU  - Prudencio, Miguel
AU  - Sciotii, Richard J.
AU  - Pečić, Stevan
AU  - D'Alessandro, Sarah
AU  - Taramelli, Donatella
AU  - Šolaja, Bogdan A.
PY  - 2016
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/3606
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - Supplementary data for the article: Terzić, N.; Konstantinović, J.; Tot, M.; Burojević, J.; Djurković-Djaković, O.; Srbljanović, J.; Štajner, T.; Verbić, T.; Zlatović, M.; Machado, M.; et al. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? Journal of Medicinal Chemistry 2016, 59 (1), 264–281. https://doi.org/10.1021/acs.jmedchem.5b01374
ER  - 
@book{
author = "Terzić-Jovanović, Nataša and Konstantinović, Jelena M. and Tot, Mikloš and Burojević, Jovana and Đurković-Đaković, Olgica and Srbljanović, Jelena and Štajner, Tijana and Verbić, Tatjana and Zlatović, Mario and Machado, Marta and Albuquerque, Ines S. and Prudencio, Miguel and Sciotii, Richard J. and Pečić, Stevan and D'Alessandro, Sarah and Taramelli, Donatella and Šolaja, Bogdan A.",
year = "2016",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/3606",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "Supplementary data for the article: Terzić, N.; Konstantinović, J.; Tot, M.; Burojević, J.; Djurković-Djaković, O.; Srbljanović, J.; Štajner, T.; Verbić, T.; Zlatović, M.; Machado, M.; et al. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? Journal of Medicinal Chemistry 2016, 59 (1), 264–281. https://doi.org/10.1021/acs.jmedchem.5b01374"
}
Terzić-Jovanović, N., Konstantinović, J. M., Tot, M., Burojević, J., Đurković-Đaković, O., Srbljanović, J., Štajner, T., Verbić, T., Zlatović, M., Machado, M., Albuquerque, I. S., Prudencio, M., Sciotii, R. J., Pečić, S., D'Alessandro, S., Taramelli, D.,& Šolaja, B. A. (2016). Supplementary data for the article: Terzić, N.; Konstantinović, J.; Tot, M.; Burojević, J.; Djurković-Djaković, O.; Srbljanović, J.; Štajner, T.; Verbić, T.; Zlatović, M.; Machado, M.; et al. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? Journal of Medicinal Chemistry 2016, 59 (1), 264–281. https://doi.org/10.1021/acs.jmedchem.5b01374.
Journal of Medicinal Chemistry
Amer Chemical Soc, Washington..
Terzić-Jovanović N, Konstantinović JM, Tot M, Burojević J, Đurković-Đaković O, Srbljanović J, Štajner T, Verbić T, Zlatović M, Machado M, Albuquerque IS, Prudencio M, Sciotii RJ, Pečić S, D'Alessandro S, Taramelli D, Šolaja BA. Supplementary data for the article: Terzić, N.; Konstantinović, J.; Tot, M.; Burojević, J.; Djurković-Djaković, O.; Srbljanović, J.; Štajner, T.; Verbić, T.; Zlatović, M.; Machado, M.; et al. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? Journal of Medicinal Chemistry 2016, 59 (1), 264–281. https://doi.org/10.1021/acs.jmedchem.5b01374. Journal of Medicinal Chemistry. 2016;
Terzić-Jovanović Nataša, Konstantinović Jelena M., Tot Mikloš, Burojević Jovana, Đurković-Đaković Olgica, Srbljanović Jelena, Štajner Tijana, Verbić Tatjana, Zlatović Mario, Machado Marta, Albuquerque Ines S., Prudencio Miguel, Sciotii Richard J., Pečić Stevan, D'Alessandro Sarah, Taramelli Donatella, Šolaja Bogdan A., "Supplementary data for the article: Terzić, N.; Konstantinović, J.; Tot, M.; Burojević, J.; Djurković-Djaković, O.; Srbljanović, J.; Štajner, T.; Verbić, T.; Zlatović, M.; Machado, M.; et al. Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials? Journal of Medicinal Chemistry 2016, 59 (1), 264–281. https://doi.org/10.1021/acs.jmedchem.5b01374" Journal of Medicinal Chemistry (2016)

Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease and P. falciparum Malaria

Selaković, Milica; Opsenica, Dejan M.; Burnett, James C.; Gomba, Laura; Nuss, Jonathan E.; Selaković, Života; Konstantinović, Jelena M.; Krstić-Ristivojević, Maja; Šegan, Sandra B.; Zlatović, Mario; Sciotti, Richard J.; Bavari, Sina; Šolaja, Bogdan A.

(Amer Chemical Soc, Washington, 2014)

TY  - JOUR
AU  - Selaković, Milica
AU  - Opsenica, Dejan M.
AU  - Burnett, James C.
AU  - Gomba, Laura
AU  - Nuss, Jonathan E.
AU  - Selaković, Života
AU  - Konstantinović, Jelena M.
AU  - Krstić-Ristivojević, Maja
AU  - Šegan, Sandra B.
AU  - Zlatović, Mario
AU  - Sciotti, Richard J.
AU  - Bavari, Sina
AU  - Šolaja, Bogdan A.
PY  - 2014
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/1781
AB  - Significantly more potent second generation 4-amino-7-chloroquinoline (4,7-ACQ) based inhibitors of the botulinum neurotoxin serotype A (BoNT/A) light chain were synthesized. Introducing an amino group at the C(3) position of the cholate component markedly increased potency (IC50 values for such derivatives ranged from 0.81 to 2.27 mu M). Two additional subclasses were prepared: bis(steroidal)-4,7-ACQ derivatives and bis(4,7-ACQ)cholate derivatives; both classes provided inhibitors with nanomolar-range potencies (e.g., the K-i of compound 67 is 0.10 mu M). During BoNT/A challenge using primary neurons, select derivatives protected SNAP-25 by up to 89%. Docking simulations were performed to rationalize the compounds' in vitro potencies. In addition to specific residue contacts, coordination of the enzyme's catalytic zinc and expulsion of the enzyme's catalytic water were a consistent theme. With respect to antimalarial activity, the compounds provided better IC90 activities against chloroquine resistant (CQR) malaria than CQ, and seven compounds were more active than mefloquine against CQR strain W2.
PB  - Amer Chemical Soc, Washington
T2  - Journal of Medicinal Chemistry
T1  - Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease and P. falciparum Malaria
VL  - 57
IS  - 10
SP  - 4134
EP  - 4153
DO  - 10.1021/jm500033r
ER  - 
@article{
author = "Selaković, Milica and Opsenica, Dejan M. and Burnett, James C. and Gomba, Laura and Nuss, Jonathan E. and Selaković, Života and Konstantinović, Jelena M. and Krstić-Ristivojević, Maja and Šegan, Sandra B. and Zlatović, Mario and Sciotti, Richard J. and Bavari, Sina and Šolaja, Bogdan A.",
year = "2014",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/1781",
abstract = "Significantly more potent second generation 4-amino-7-chloroquinoline (4,7-ACQ) based inhibitors of the botulinum neurotoxin serotype A (BoNT/A) light chain were synthesized. Introducing an amino group at the C(3) position of the cholate component markedly increased potency (IC50 values for such derivatives ranged from 0.81 to 2.27 mu M). Two additional subclasses were prepared: bis(steroidal)-4,7-ACQ derivatives and bis(4,7-ACQ)cholate derivatives; both classes provided inhibitors with nanomolar-range potencies (e.g., the K-i of compound 67 is 0.10 mu M). During BoNT/A challenge using primary neurons, select derivatives protected SNAP-25 by up to 89%. Docking simulations were performed to rationalize the compounds' in vitro potencies. In addition to specific residue contacts, coordination of the enzyme's catalytic zinc and expulsion of the enzyme's catalytic water were a consistent theme. With respect to antimalarial activity, the compounds provided better IC90 activities against chloroquine resistant (CQR) malaria than CQ, and seven compounds were more active than mefloquine against CQR strain W2.",
publisher = "Amer Chemical Soc, Washington",
journal = "Journal of Medicinal Chemistry",
title = "Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease and P. falciparum Malaria",
volume = "57",
number = "10",
pages = "4134-4153",
doi = "10.1021/jm500033r"
}
Selaković, M., Opsenica, D. M., Burnett, J. C., Gomba, L., Nuss, J. E., Selaković, Ž., Konstantinović, J. M., Krstić-Ristivojević, M., Šegan, S. B., Zlatović, M., Sciotti, R. J., Bavari, S.,& Šolaja, B. A. (2014). Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease and P. falciparum Malaria.
Journal of Medicinal Chemistry
Amer Chemical Soc, Washington., 57(10), 4134-4153.
https://doi.org/10.1021/jm500033r
Selaković M, Opsenica DM, Burnett JC, Gomba L, Nuss JE, Selaković Ž, Konstantinović JM, Krstić-Ristivojević M, Šegan SB, Zlatović M, Sciotti RJ, Bavari S, Šolaja BA. Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease and P. falciparum Malaria. Journal of Medicinal Chemistry. 2014;57(10):4134-4153
Selaković Milica, Opsenica Dejan M., Burnett James C., Gomba Laura, Nuss Jonathan E., Selaković Života, Konstantinović Jelena M., Krstić-Ristivojević Maja, Šegan Sandra B., Zlatović Mario, Sciotti Richard J., Bavari Sina, Šolaja Bogdan A., "Second Generation Steroidal 4-Aminoquinolines Are Potent, Dual-Target Inhibitors of the Botulinum Neurotoxin Serotype A Metalloprotease and P. falciparum Malaria" Journal of Medicinal Chemistry, 57, no. 10 (2014):4134-4153,
https://doi.org/10.1021/jm500033r .
3
22
21
26

Botox as the medication: Usage and abuse

Lupović, Danijela; Konstantinović, Jelena M.

(2010)

TY  - JOUR
AU  - Lupović, Danijela
AU  - Konstantinović, Jelena M.
PY  - 2010
UR  - http://cherry.chem.bg.ac.rs/handle/123456789/275
AB  - Botulinum toxin is a neurotoxic protein, produced by bacterium Clostridium botulinum. This toxin specifically cleaves the SNAP-25 protein, required for vesicle fusion, that releases neurotransmitters from the axon endings (in particular acetylcholine). Although botulinum toxin is a lethal naturally occurring substance, it can be used as an effective and powerful medication, in the treatment of different types of spasms and dystonias, and also in cosmetics, but potential side effects do exist. Commercially it is known as BotoxR.
AB  - Botulinski toksin je izuzetno otrovna supstanca koju proizvodi bakterija Clostridum botulinum. Deluje na periferne nervne završetke, blokirajući oslobađanje neurotransmitera acetilholina. Interesantan je po tome što može da izazove oboljenje (botulizam), ali i da služi za lečenje mnogih bolesti (na primer, cervikalna distonija). U današnje vreme se koristi u različitim kozmetičkim tretmanima. Prekomerna upotreba izaziva neželjene efekte, a može dovesti do smrti.
T2  - Hemijski pregled
T1  - Botox as the medication: Usage and abuse
T1  - Botoks - upotreba i zloupotreba
VL  - 51
IS  - 5
SP  - 118
EP  - 120
ER  - 
@article{
author = "Lupović, Danijela and Konstantinović, Jelena M.",
year = "2010",
url = "http://cherry.chem.bg.ac.rs/handle/123456789/275",
abstract = "Botulinum toxin is a neurotoxic protein, produced by bacterium Clostridium botulinum. This toxin specifically cleaves the SNAP-25 protein, required for vesicle fusion, that releases neurotransmitters from the axon endings (in particular acetylcholine). Although botulinum toxin is a lethal naturally occurring substance, it can be used as an effective and powerful medication, in the treatment of different types of spasms and dystonias, and also in cosmetics, but potential side effects do exist. Commercially it is known as BotoxR., Botulinski toksin je izuzetno otrovna supstanca koju proizvodi bakterija Clostridum botulinum. Deluje na periferne nervne završetke, blokirajući oslobađanje neurotransmitera acetilholina. Interesantan je po tome što može da izazove oboljenje (botulizam), ali i da služi za lečenje mnogih bolesti (na primer, cervikalna distonija). U današnje vreme se koristi u različitim kozmetičkim tretmanima. Prekomerna upotreba izaziva neželjene efekte, a može dovesti do smrti.",
journal = "Hemijski pregled",
title = "Botox as the medication: Usage and abuse, Botoks - upotreba i zloupotreba",
volume = "51",
number = "5",
pages = "118-120"
}
Lupović, D.,& Konstantinović, J. M. (2010). Botoks - upotreba i zloupotreba.
Hemijski pregled, 51(5), 118-120.
Lupović D, Konstantinović JM. Botoks - upotreba i zloupotreba. Hemijski pregled. 2010;51(5):118-120
Lupović Danijela, Konstantinović Jelena M., "Botoks - upotreba i zloupotreba" Hemijski pregled, 51, no. 5 (2010):118-120