Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
Аутори
Konstantinović, Jelena M.Videnović, Milica
Orsini, Stefania
Bogojević, Katarina
D'Alessandro, Sarah
Scaccabarozzi, Diletta
Terzić-Jovanović, Nataša
Gradoni, Luigi
Basilico, Nicoletta
Šolaja, Bogdan A.
Чланак у часопису (Рецензирана верзија)
Метаподаци
Приказ свих података о документуАпстракт
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.
Кључне речи:
Leishmania infantum / promastigote / amastigote / mice model / aminoquinolineИзвор:
ACS Medicinal Chemistry Letters, 2018, 9, 7, 629-634Издавач:
- Amer Chemical Soc, Washington
Финансирање / пројекти:
- Синтеза аминохинолина и њихових деривата као антималарика и инхибитора ботулинум неуротоксина А (RS-MESTD-Basic Research (BR or ON)-172008)
- 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
Напомена:
- This is the peer-reviewed version of the following 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
- Sipplementary material: http://cherry.chem.bg.ac.rs/handle/123456789/2949
DOI: 10.1021/acsmedchemlett.8b00053
ISSN: 1948-5875
PubMed: 30034591
WoS: 000442964000011
Scopus: 2-s2.0-85046787760
Колекције
Институција/група
Hemijski fakultet / Faculty of ChemistryTY - JOUR AU - Konstantinović, Jelena M. AU - Videnović, 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 - https://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 Videnović, 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", 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., Videnović, 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. in ACS Medicinal Chemistry Letters Amer Chemical Soc, Washington., 9(7), 629-634. https://doi.org/10.1021/acsmedchemlett.8b00053
Konstantinović JM, Videnović 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. in ACS Medicinal Chemistry Letters. 2018;9(7):629-634. doi:10.1021/acsmedchemlett.8b00053 .
Konstantinović, Jelena M., Videnović, 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" in ACS Medicinal Chemistry Letters, 9, no. 7 (2018):629-634, https://doi.org/10.1021/acsmedchemlett.8b00053 . .