858466-68-9Relevant academic research and scientific papers
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.
