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

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 < 1 μM against promastigote stages of L. infantum and L. tropica, and five compounds showed IC50 < 1 μM 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.

SUBMITTER: Konstantinovic J 

PROVIDER: S-EPMC6047044 | biostudies-other | 2018 Jul

REPOSITORIES: biostudies-other

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Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in <i>Leishmania infantum</i> Infected Mice.

Konstantinović Jelena J   Videnović Milica M   Orsini Stefania S   Bogojević Katarina K   D'Alessandro Sarah S   Scaccabarozzi Diletta D   Terzić Jovanović Nataša N   Gradoni Luigi L   Basilico Nicoletta N   Šolaja Bogdan A BA  

ACS medicinal chemistry letters 20180504 7

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 IC<sub>50</sub> < 1 μM against promastigote stages of <i>L. infantum</i> and <i>L. tropica</i>, and five compounds showed IC<sub>50</sub> < 1 μM against intramacrophage <i>L. infantum</i> amastigotes. Two compounds showed dose-dependent enhancement of NO and ROS production by bone marrow-derived macrophages and remarka  ...[more]