TY  - JOUR
AU  - Opsenica, Igor
AU  - Selaković, Milica
AU  - Tot, Mikloš
AU  - Verbić, Tatjana
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Đurković-Đaković, Olgica
AU  - Šolaja, Bogdan A.
PY  - 2021
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/4389
AB  - Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three aminoquinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Antimalarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured. © 2021 Serbian Chemical Society. All rights reserved.
PB  - Belgrade : Serbian Chemical Society
T2  - Journal of the Serbian Chemical Society
T1  - New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria
VL  - 86
IS  - 2
SP  - 115
EP  - 123
DO  - 10.2298/JSC201225005O
ER  - 

@article{
author = "Opsenica, Igor and Selaković, Milica and Tot, Mikloš and Verbić, Tatjana and Srbljanović, Jelena and Štajner, Tijana and Đurković-Đaković, Olgica and Šolaja, Bogdan A.",
year = "2021",
abstract = "Synthesis of novel aminoquinoline derivatives has been accomplished and their activity against malaria strains has been examined. The compounds showed moderate in vitro antimalarial activity against two P. falciparum strains, 3D7 (CQ susceptible clone) and Dd2 (CQ resistant clone). Three aminoquinolines were further examined for antimalarial efficacy in a mouse model using a modified Thompson test. In this model, mice were infected with P. berghei-infected red blood cells, and drugs were administered orally. Antimalarial 3 was found toxic at a dose of 320 (mg/kg)/day in 3/6 mice, however, 2/6 mice of the same group survived through day 31, and one of them was cured. © 2021 Serbian Chemical Society. All rights reserved.",
publisher = "Belgrade : Serbian Chemical Society",
journal = "Journal of the Serbian Chemical Society",
title = "New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria",
volume = "86",
number = "2",
pages = "115-123",
doi = "10.2298/JSC201225005O"
}

Opsenica, I., Selaković, M., Tot, M., Verbić, T., Srbljanović, J., Štajner, T., Đurković-Đaković, O.,& Šolaja, B. A.. (2021). New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria. in Journal of the Serbian Chemical Society
Belgrade : Serbian Chemical Society., 86(2), 115-123.
https://doi.org/10.2298/JSC201225005O

Opsenica I, Selaković M, Tot M, Verbić T, Srbljanović J, Štajner T, Đurković-Đaković O, Šolaja BA. New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria. in Journal of the Serbian Chemical Society. 2021;86(2):115-123.
doi:10.2298/JSC201225005O .

Opsenica, Igor, Selaković, Milica, Tot, Mikloš, Verbić, Tatjana, Srbljanović, Jelena, Štajner, Tijana, Đurković-Đaković, Olgica, Šolaja, Bogdan A., "New 4-aminoquinolines as moderate inhibitors of P. falciparum malaria" in Journal of the Serbian Chemical Society, 86, no. 2 (2021):115-123,
https://doi.org/10.2298/JSC201225005O . .

TY  - DATA
AU  - Opsenica, Igor
AU  - Selaković, Milica
AU  - Tot, Mikloš
AU  - Verbić, Tatjana
AU  - Srbljanović, Jelena
AU  - Štajner, Tijana
AU  - Đurković-Đaković, Olgica
AU  - Šolaja, Bogdan A.
PY  - 2021
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/4392
PB  - Belgrade : Serbian Chemical Society
T2  - Journal of the Serbian Chemical Society
T1  - Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O
VL  - 86
IS  - 2
UR  - https://hdl.handle.net/21.15107/rcub_cherry_4392
ER  - 

@misc{
author = "Opsenica, Igor and Selaković, Milica and Tot, Mikloš and Verbić, Tatjana and Srbljanović, Jelena and Štajner, Tijana and Đurković-Đaković, Olgica and Šolaja, Bogdan A.",
year = "2021",
publisher = "Belgrade : Serbian Chemical Society",
journal = "Journal of the Serbian Chemical Society",
title = "Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O",
volume = "86",
number = "2",
url = "https://hdl.handle.net/21.15107/rcub_cherry_4392"
}

Opsenica, I., Selaković, M., Tot, M., Verbić, T., Srbljanović, J., Štajner, T., Đurković-Đaković, O.,& Šolaja, B. A.. (2021). Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O. in Journal of the Serbian Chemical Society
Belgrade : Serbian Chemical Society., 86(2).
https://hdl.handle.net/21.15107/rcub_cherry_4392

Opsenica I, Selaković M, Tot M, Verbić T, Srbljanović J, Štajner T, Đurković-Đaković O, Šolaja BA. Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O. in Journal of the Serbian Chemical Society. 2021;86(2).
https://hdl.handle.net/21.15107/rcub_cherry_4392 .

Opsenica, Igor, Selaković, Milica, Tot, Mikloš, Verbić, Tatjana, Srbljanović, Jelena, Štajner, Tijana, Đurković-Đaković, Olgica, Šolaja, Bogdan A., "Supplementary data for the article: Opsenica, I.; Selaković, M.; Tot, M.; Verbić, T.; Srbljanović, J.; Štajner, T.; Djaković, O. D.; Šolaja, B. A. New 4-Aminoquinolines as Moderate Inhibitors of P. Falciparum Malaria. J. Serb. Chem. Soc. 2021, 86 (2), 115–123. https://doi.org/10.2298/JSC201225005O" in Journal of the Serbian Chemical Society, 86, no. 2 (2021),
https://hdl.handle.net/21.15107/rcub_cherry_4392 .

TY  - JOUR
AU  - Srbljanović, Jelena
AU  - Bobić, Branko
AU  - Štajner, Tijana
AU  - Uzelac, Aleksandra
AU  - Opsenica, Igor
AU  - Terzić-Jovanović, Nataša
AU  - Bauman, Neda
AU  - Šolaja, Bogdan A.
AU  - Đurković-Đaković, Olgica
PY  - 2020
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/4054
AB  - ObjectivesMalaria treatment is impeded by increasing resistance to conventional antimalarial drugs. Here we explored the activity of ten novel benzothiophene, thiophene and benzene aminoquinolines.MethodsIn vitro testing was performed by the lactate dehydrogenase assay in chloroquine (CQ)-sensitive Plasmodium falciparum strain 3D7 and CQ-resistant (CQR) P. falciparum strain Dd2. In vivo activity was evaluated by a modified Thompson test using C57BL/6 mice infected with Plasmodium berghei ANKA strain.ResultsNine of the ten compounds had a lower 50% inhibitory concentration (IC50) than CQ against the CQR strain Dd2. Five of these compounds that were available for in vivo evaluation were shown to be non-toxic. All five compounds administered at a dose of 160mg/kg/day for 3 days prolonged the survival of treated compared with untreated mice. Untreated control mice died by Day 7 with a mean parasitaemia of 15%. Among treated mice, a dichotomous outcome was observed, with a two-third majority of treated mice dying by Day 17 with a low mean parasitaemia of 5%, whilst one-third survived longer with a mean hyperparasitaemia of 70%; specifically, five of these mice survived a mean of 25 days, whilst two even survived past Day 31.ConclusionsThe significant antimalarial potential of this aminoquinoline series is illustrated by its excellent in vitro activity against the CQR P. falciparum strain and significant in vivo activity. Interestingly, compounds ClAQ7, ClAQ9 and ClAQ11 were able to confer resistance to cerebral malaria and afford a switch to hyperparasitaemia to mice prone to the neurological syndrome.
PB  - Elsevier
T2  - Journal of Global Antimicrobial Resistance
T2  - Journal of Global Antimicrobial Resistance
T1  - Aminoquinolines afford resistance to cerebral malaria in susceptible mice
VL  - 23
SP  - 20
EP  - 25
DO  - 10.1016/j.jgar.2020.07.027
ER  - 

@article{
author = "Srbljanović, Jelena and Bobić, Branko and Štajner, Tijana and Uzelac, Aleksandra and Opsenica, Igor and Terzić-Jovanović, Nataša and Bauman, Neda and Šolaja, Bogdan A. and Đurković-Đaković, Olgica",
year = "2020",
abstract = "ObjectivesMalaria treatment is impeded by increasing resistance to conventional antimalarial drugs. Here we explored the activity of ten novel benzothiophene, thiophene and benzene aminoquinolines.MethodsIn vitro testing was performed by the lactate dehydrogenase assay in chloroquine (CQ)-sensitive Plasmodium falciparum strain 3D7 and CQ-resistant (CQR) P. falciparum strain Dd2. In vivo activity was evaluated by a modified Thompson test using C57BL/6 mice infected with Plasmodium berghei ANKA strain.ResultsNine of the ten compounds had a lower 50% inhibitory concentration (IC50) than CQ against the CQR strain Dd2. Five of these compounds that were available for in vivo evaluation were shown to be non-toxic. All five compounds administered at a dose of 160mg/kg/day for 3 days prolonged the survival of treated compared with untreated mice. Untreated control mice died by Day 7 with a mean parasitaemia of 15%. Among treated mice, a dichotomous outcome was observed, with a two-third majority of treated mice dying by Day 17 with a low mean parasitaemia of 5%, whilst one-third survived longer with a mean hyperparasitaemia of 70%; specifically, five of these mice survived a mean of 25 days, whilst two even survived past Day 31.ConclusionsThe significant antimalarial potential of this aminoquinoline series is illustrated by its excellent in vitro activity against the CQR P. falciparum strain and significant in vivo activity. Interestingly, compounds ClAQ7, ClAQ9 and ClAQ11 were able to confer resistance to cerebral malaria and afford a switch to hyperparasitaemia to mice prone to the neurological syndrome.",
publisher = "Elsevier",
journal = "Journal of Global Antimicrobial Resistance, Journal of Global Antimicrobial Resistance",
title = "Aminoquinolines afford resistance to cerebral malaria in susceptible mice",
volume = "23",
pages = "20-25",
doi = "10.1016/j.jgar.2020.07.027"
}

Srbljanović, J., Bobić, B., Štajner, T., Uzelac, A., Opsenica, I., Terzić-Jovanović, N., Bauman, N., Šolaja, B. A.,& Đurković-Đaković, O.. (2020). Aminoquinolines afford resistance to cerebral malaria in susceptible mice. in Journal of Global Antimicrobial Resistance
Elsevier., 23, 20-25.
https://doi.org/10.1016/j.jgar.2020.07.027

Srbljanović J, Bobić B, Štajner T, Uzelac A, Opsenica I, Terzić-Jovanović N, Bauman N, Šolaja BA, Đurković-Đaković O. Aminoquinolines afford resistance to cerebral malaria in susceptible mice. in Journal of Global Antimicrobial Resistance. 2020;23:20-25.
doi:10.1016/j.jgar.2020.07.027 .

Srbljanović, Jelena, Bobić, Branko, Štajner, Tijana, Uzelac, Aleksandra, Opsenica, Igor, Terzić-Jovanović, Nataša, Bauman, Neda, Šolaja, Bogdan A., Đurković-Đaković, Olgica, "Aminoquinolines afford resistance to cerebral malaria in susceptible mice" in Journal of Global Antimicrobial Resistance, 23 (2020):20-25,
https://doi.org/10.1016/j.jgar.2020.07.027 . .

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  - https://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",
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. in 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. in International Journal of Antimicrobial Agents. 2017;50(3):461-466.
doi:10.1016/j.ijantimicag.2017.06.002 .

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" in International Journal of Antimicrobial Agents, 50, no. 3 (2017):461-466,
https://doi.org/10.1016/j.ijantimicag.2017.06.002 . .

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  - https://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",
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. in 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. in International Journal of Antimicrobial Agents. 2017;50(3):461-466.
doi:10.1016/j.ijantimicag.2017.06.002 .

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" in International Journal of Antimicrobial Agents, 50, no. 3 (2017):461-466,
https://doi.org/10.1016/j.ijantimicag.2017.06.002 . .

TY  - JOUR
AU  - Konstantinović, Jelena M.
AU  - Videnović, Milica
AU  - Srbljanović, Jelena
AU  - Đurković-Đaković, Olgica
AU  - Bogojević, Katarina
AU  - Sciotti, Richard J.
AU  - Šolaja, Bogdan A.
PY  - 2017
UR  - https://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 Videnović, Milica and Srbljanović, Jelena and Đurković-Đaković, Olgica and Bogojević, Katarina and Sciotti, Richard J. and Šolaja, Bogdan A.",
year = "2017",
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., Videnović, M., Srbljanović, J., Đurković-Đaković, O., Bogojević, K., Sciotti, R. J.,& Šolaja, B. A.. (2017). Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. in Molecules
Mdpi Ag, Basel., 22(3).
https://doi.org/10.3390/molecules22030343

Konstantinović JM, Videnović M, Srbljanović J, Đurković-Đaković O, Bogojević K, Sciotti RJ, Šolaja BA. Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners. in Molecules. 2017;22(3).
doi:10.3390/molecules22030343 .

Konstantinović, Jelena M., Videnović, Milica, Srbljanović, Jelena, Đurković-Đaković, Olgica, Bogojević, Katarina, Sciotti, Richard J., Šolaja, Bogdan A., "Antimalarials with Benzothiophene Moieties as Aminoquinoline Partners" in Molecules, 22, no. 3 (2017),
https://doi.org/10.3390/molecules22030343 . .

TY  - DATA
AU  - Konstantinović, Jelena M.
AU  - Videnović, Milica
AU  - Srbljanović, Jelena
AU  - Đurković-Đaković, Olgica
AU  - Bogojević, Katarina
AU  - Sciotti, Richard J.
AU  - Šolaja, Bogdan A.
PY  - 2017
UR  - https://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
UR  - https://hdl.handle.net/21.15107/rcub_cherry_3022
ER  - 

@misc{
author = "Konstantinović, Jelena M. and Videnović, Milica and Srbljanović, Jelena and Đurković-Đaković, Olgica and Bogojević, Katarina and Sciotti, Richard J. and Šolaja, Bogdan A.",
year = "2017",
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",
url = "https://hdl.handle.net/21.15107/rcub_cherry_3022"
}

Konstantinović, J. M., Videnović, M., Srbljanović, J., Đurković-Đaković, O., Bogojević, K., Sciotti, R. J.,& 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. in Molecules
Mdpi Ag, Basel..
https://hdl.handle.net/21.15107/rcub_cherry_3022

Konstantinović JM, Videnović M, Srbljanović J, Đurković-Đaković O, Bogojević K, Sciotti RJ, 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. in Molecules. 2017;.
https://hdl.handle.net/21.15107/rcub_cherry_3022 .

Konstantinović, Jelena M., Videnović, Milica, Srbljanović, Jelena, Đurković-Đaković, Olgica, Bogojević, Katarina, Sciotti, Richard J., 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" in Molecules (2017),
https://hdl.handle.net/21.15107/rcub_cherry_3022 .

TY  - DATA
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  - https://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
UR  - https://hdl.handle.net/21.15107/rcub_cherry_3606
ER  - 

@misc{
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",
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",
url = "https://hdl.handle.net/21.15107/rcub_cherry_3606"
}

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. in Journal of Medicinal Chemistry
Amer Chemical Soc, Washington..
https://hdl.handle.net/21.15107/rcub_cherry_3606

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. in Journal of Medicinal Chemistry. 2016;.
https://hdl.handle.net/21.15107/rcub_cherry_3606 .

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" in Journal of Medicinal Chemistry (2016),
https://hdl.handle.net/21.15107/rcub_cherry_3606 .

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  - https://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",
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?. in 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?. in Journal of Medicinal Chemistry. 2016;59(1):264-281.
doi: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., "Reinvestigating Old Pharmacophores: Are 4-Aminoquinolines and Tetraoxanes Potential Two-Stage Antimalarials?" in Journal of Medicinal Chemistry, 59, no. 1 (2016):264-281,
https://doi.org/10.1021/acs.jmedchem.5b01374 . .

TY  - DATA
AU  - Opsenica, Igor
AU  - Verbić, Tatjana
AU  - Tot, Mikloš
AU  - Sciotti, Richard J.
AU  - Pybus, Brandon S.
AU  - Đurković-Đaković, Olgica
AU  - Slavić, Ksenija
AU  - Šolaja, Bogdan A.
PY  - 2015
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/3381
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Bioorganic and Medicinal Chemistry
T1  - Supplementary data for article: Opsenica, I. M.; Verbić, T. Ž.; Tot, M.; Sciotti, R. J.; Pybus, B. S.; Djurković-Djaković, O.; Slavić, K.; Šolaja, B. A. Investigation into Novel Thiophene- and Furan-Based 4-Amino-7-Chloroquinolines Afforded Antimalarials That Cure Mice. Bioorganic and Medicinal Chemistry 2015, 23 (9), 2176–2186. https://doi.org/10.1016/j.bmc.2015.02.061
UR  - https://hdl.handle.net/21.15107/rcub_cherry_3381
ER  - 

@misc{
author = "Opsenica, Igor and Verbić, Tatjana and Tot, Mikloš and Sciotti, Richard J. and Pybus, Brandon S. and Đurković-Đaković, Olgica and Slavić, Ksenija and Šolaja, Bogdan A.",
year = "2015",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Bioorganic and Medicinal Chemistry",
title = "Supplementary data for article: Opsenica, I. M.; Verbić, T. Ž.; Tot, M.; Sciotti, R. J.; Pybus, B. S.; Djurković-Djaković, O.; Slavić, K.; Šolaja, B. A. Investigation into Novel Thiophene- and Furan-Based 4-Amino-7-Chloroquinolines Afforded Antimalarials That Cure Mice. Bioorganic and Medicinal Chemistry 2015, 23 (9), 2176–2186. https://doi.org/10.1016/j.bmc.2015.02.061",
url = "https://hdl.handle.net/21.15107/rcub_cherry_3381"
}

Opsenica, I., Verbić, T., Tot, M., Sciotti, R. J., Pybus, B. S., Đurković-Đaković, O., Slavić, K.,& Šolaja, B. A.. (2015). Supplementary data for article: Opsenica, I. M.; Verbić, T. Ž.; Tot, M.; Sciotti, R. J.; Pybus, B. S.; Djurković-Djaković, O.; Slavić, K.; Šolaja, B. A. Investigation into Novel Thiophene- and Furan-Based 4-Amino-7-Chloroquinolines Afforded Antimalarials That Cure Mice. Bioorganic and Medicinal Chemistry 2015, 23 (9), 2176–2186. https://doi.org/10.1016/j.bmc.2015.02.061. in Bioorganic and Medicinal Chemistry
Pergamon-Elsevier Science Ltd, Oxford..
https://hdl.handle.net/21.15107/rcub_cherry_3381

Opsenica I, Verbić T, Tot M, Sciotti RJ, Pybus BS, Đurković-Đaković O, Slavić K, Šolaja BA. Supplementary data for article: Opsenica, I. M.; Verbić, T. Ž.; Tot, M.; Sciotti, R. J.; Pybus, B. S.; Djurković-Djaković, O.; Slavić, K.; Šolaja, B. A. Investigation into Novel Thiophene- and Furan-Based 4-Amino-7-Chloroquinolines Afforded Antimalarials That Cure Mice. Bioorganic and Medicinal Chemistry 2015, 23 (9), 2176–2186. https://doi.org/10.1016/j.bmc.2015.02.061. in Bioorganic and Medicinal Chemistry. 2015;.
https://hdl.handle.net/21.15107/rcub_cherry_3381 .

Opsenica, Igor, Verbić, Tatjana, Tot, Mikloš, Sciotti, Richard J., Pybus, Brandon S., Đurković-Đaković, Olgica, Slavić, Ksenija, Šolaja, Bogdan A., "Supplementary data for article: Opsenica, I. M.; Verbić, T. Ž.; Tot, M.; Sciotti, R. J.; Pybus, B. S.; Djurković-Djaković, O.; Slavić, K.; Šolaja, B. A. Investigation into Novel Thiophene- and Furan-Based 4-Amino-7-Chloroquinolines Afforded Antimalarials That Cure Mice. Bioorganic and Medicinal Chemistry 2015, 23 (9), 2176–2186. https://doi.org/10.1016/j.bmc.2015.02.061" in Bioorganic and Medicinal Chemistry (2015),
https://hdl.handle.net/21.15107/rcub_cherry_3381 .

TY  - JOUR
AU  - Opsenica, Igor
AU  - Verbić, Tatjana
AU  - Tot, Mikloš
AU  - Sciotti, Richard J.
AU  - Pybus, Brandon S.
AU  - Đurković-Đaković, Olgica
AU  - Slavić, Ksenija
AU  - Šolaja, Bogdan A.
PY  - 2015
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/1691
AB  - We herein report the design and synthesis of a novel series of thiophene-and furan-based aminoquinoline derivatives which were found to be potent antimalarials and inhibitors of b-hematin polymerization. Tested compounds were 3-71 times more potent in vitro than CQ against chloroquine-resistant (CQR) W2 strain with benzonitrile 30 being as active as mefloquine (MFQ), and almost all synthesized aminoquinolines (22/27) were more potent than MFQ against multidrug-resistant (MDR) strain C235. In vivo experiments revealed that compound 28 showed clearance with recrudescence at 40 mg/kg/day, while 5/5 mice survived in Thompson test at 160 mg/kg/day.
PB  - Pergamon-Elsevier Science Ltd, Oxford
T2  - Bioorganic and Medicinal Chemistry
T1  - Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice
VL  - 23
IS  - 9
SP  - 2176
EP  - 2186
DO  - 10.1016/j.bmc.2015.02.061
ER  - 

@article{
author = "Opsenica, Igor and Verbić, Tatjana and Tot, Mikloš and Sciotti, Richard J. and Pybus, Brandon S. and Đurković-Đaković, Olgica and Slavić, Ksenija and Šolaja, Bogdan A.",
year = "2015",
abstract = "We herein report the design and synthesis of a novel series of thiophene-and furan-based aminoquinoline derivatives which were found to be potent antimalarials and inhibitors of b-hematin polymerization. Tested compounds were 3-71 times more potent in vitro than CQ against chloroquine-resistant (CQR) W2 strain with benzonitrile 30 being as active as mefloquine (MFQ), and almost all synthesized aminoquinolines (22/27) were more potent than MFQ against multidrug-resistant (MDR) strain C235. In vivo experiments revealed that compound 28 showed clearance with recrudescence at 40 mg/kg/day, while 5/5 mice survived in Thompson test at 160 mg/kg/day.",
publisher = "Pergamon-Elsevier Science Ltd, Oxford",
journal = "Bioorganic and Medicinal Chemistry",
title = "Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice",
volume = "23",
number = "9",
pages = "2176-2186",
doi = "10.1016/j.bmc.2015.02.061"
}

Opsenica, I., Verbić, T., Tot, M., Sciotti, R. J., Pybus, B. S., Đurković-Đaković, O., Slavić, K.,& Šolaja, B. A.. (2015). Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice. in Bioorganic and Medicinal Chemistry
Pergamon-Elsevier Science Ltd, Oxford., 23(9), 2176-2186.
https://doi.org/10.1016/j.bmc.2015.02.061

Opsenica I, Verbić T, Tot M, Sciotti RJ, Pybus BS, Đurković-Đaković O, Slavić K, Šolaja BA. Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice. in Bioorganic and Medicinal Chemistry. 2015;23(9):2176-2186.
doi:10.1016/j.bmc.2015.02.061 .

Opsenica, Igor, Verbić, Tatjana, Tot, Mikloš, Sciotti, Richard J., Pybus, Brandon S., Đurković-Đaković, Olgica, Slavić, Ksenija, Šolaja, Bogdan A., "Investigation into novel thiophene- and furan-based 4-amino-7-chloroquinolines afforded antimalarials that cure mice" in Bioorganic and Medicinal Chemistry, 23, no. 9 (2015):2176-2186,
https://doi.org/10.1016/j.bmc.2015.02.061 . .

TY  - JOUR
AU  - Opsenica, Dejan M.
AU  - Radivojević, Jelena
AU  - Matić, Ivana Z.
AU  - Štajner, Tijana
AU  - Knezevic-Usaj, Slavica
AU  - Đurković-Đaković, Olgica
AU  - Šolaja, Bogdan A.
PY  - 2015
UR  - https://cherry.chem.bg.ac.rs/handle/123456789/2010
AB  - New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50  gt  200 mu M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg(-1) day(-1) for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of apicomplexan parasites.
PB  - Serbian Chemical Soc, Belgrade
T2  - Journal of the Serbian Chemical Society
T1  - Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules
VL  - 80
IS  - 11
SP  - 1339
DO  - 10.2298/JSC150430063O
ER  - 

@article{
author = "Opsenica, Dejan M. and Radivojević, Jelena and Matić, Ivana Z. and Štajner, Tijana and Knezevic-Usaj, Slavica and Đurković-Đaković, Olgica and Šolaja, Bogdan A.",
year = "2015",
abstract = "New cyclohexylidene 1,2,4,5-tetraoxanes with polar guanidine and urea based groups were synthesized and evaluated for their antimalarial activity against chloroquine resistant and susceptible Plasmodium falciparum strains. The derivatives showed moderate, nM range antimalarial activities and low cytotoxicity. The N-phenylurea derivative 24 exhibited the best resistance indices (RIW2 = 0.44, RITM91C235 = 0.80) and was not toxic against human normal peripheral blood mononuclear cells (IC50  gt  200 mu M). Seven derivatives were tested in vitro against four human cancer cell lines and they demonstrated high selectivity toward leukaemia K562 cells. One compound, derivative 21 with a primary amino group, was the first tetraoxane tested in vivo against Toxoplasma gondii as another apicomplexan parasite. Subcutaneous administration at a dose of 10 mg kg(-1) day(-1) for 8 days allowed the survival of 20 % of infected mice, thus demonstrating the high potential of tetraoxanes for the treatment of apicomplexan parasites.",
publisher = "Serbian Chemical Soc, Belgrade",
journal = "Journal of the Serbian Chemical Society",
title = "Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules",
volume = "80",
number = "11",
pages = "1339",
doi = "10.2298/JSC150430063O"
}

Opsenica, D. M., Radivojević, J., Matić, I. Z., Štajner, T., Knezevic-Usaj, S., Đurković-Đaković, O.,& Šolaja, B. A.. (2015). Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules. in Journal of the Serbian Chemical Society
Serbian Chemical Soc, Belgrade., 80(11), 1339.
https://doi.org/10.2298/JSC150430063O

Opsenica DM, Radivojević J, Matić IZ, Štajner T, Knezevic-Usaj S, Đurković-Đaković O, Šolaja BA. Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules. in Journal of the Serbian Chemical Society. 2015;80(11):1339.
doi:10.2298/JSC150430063O .

Opsenica, Dejan M., Radivojević, Jelena, Matić, Ivana Z., Štajner, Tijana, Knezevic-Usaj, Slavica, Đurković-Đaković, Olgica, Šolaja, Bogdan A., "Tetraoxanes as inhibitors of apicomplexan parasites Plasmodium falciparum and Toxoplasma gondii growth and anti-cancer molecules" in Journal of the Serbian Chemical Society, 80, no. 11 (2015):1339,
https://doi.org/10.2298/JSC150430063O . .