858466-68-9Relevant articles and documents
Novel Aminoquinoline Derivatives Significantly Reduce Parasite Load in Leishmania infantum Infected Mice
Konstantinovi?, Jelena,Videnovi?, Milica,Orsini, Stefania,Bogojevi?, Katarina,D'Alessandro, Sarah,Scaccabarozzi, Diletta,Terzi? Jovanovi?, Nata?a,Gradoni, Luigi,Basilico, Nicoletta,?olaja, Bogdan A.
, p. 629 - 634 (2018)
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 50 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.