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

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journal contribution
posted on 04.05.2018, 00:00 by Jelena Konstantinović, Milica Videnović, Stefania Orsini, Katarina Bogojević, Sarah D’Alessandro, Diletta Scaccabarozzi, Nataša Terzić Jovanović, Luigi Gradoni, Nicoletta Basilico, Bogdan A. Šolaja
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.