Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
| Autor: | Luigi Gradoni, Sarah D'Alessandro, Nicoletta Basilico, Stefania Orsini, Jelena Konstantinović, Diletta Scaccabarozzi, Milica Videnović, Bogdan A. Šolaja, Katarina Bogojević, Natasa Jovanovic |
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| Rok vydání: | 2018 |
| Předmět: |
0301 basic medicine
01 natural sciences Biochemistry Parasite load Microbiology Aminoquinoline 03 medical and health sciences In vivo parasitic diseases Drug Discovery ANTILEISHMANIAL DRUGS medicine Leishmania infantum mice model Amastigote IC50 biology 010405 organic chemistry Chemistry Organic Chemistry aminoquinoline biology.organism_classification amastigote promastigote 3. Good health 0104 chemical sciences 030104 developmental biology Orally active medicine.drug |
| Zdroj: | Acs Medicinal Chemistry Letters ACS Medicinal Chemistry Letters |
| ISSN: | 1948-5875 |
| Popis: | 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. 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] |
| Databáze: | OpenAIRE |
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