Targeting the human parasite Leishmania donovani: Discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series - Archive ouverte HAL Access content directly
Journal Articles Bioorganic and Medicinal Chemistry Year : 2013

Targeting the human parasite Leishmania donovani: Discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series

, (1, 2) , (2) , (3) , , (3) , , (3) , (4) , (3) , (5) , (4, 6) , (3) , (4)
1
2
3
4
5
6

Abstract

We report herein the discovery of antileishmanial molecules based on the imidazo[1,2-a]pyridine ring. In vitro screenings of imidazopyridines belonging to our chemical library, toward the promastigotes stage of Leishmania donovani, J774A. 1 murine and HepG2 human cells, permitted to identify three selective hit-compounds (12, 20 and 28). New derivatives were then synthesized to allow structure-activity and -toxicity relationships analyses, enabling to characterize a lead-compound (44) displaying both a high potency (IC50 = 1.8 mu M) and a good selectivity index, in comparison with three antileishmanial reference drug-compounds (amphotericin B, miltefosine and pentamidine). Moreover, lead-compound
Not file

Dates and versions

hal-01460446 , version 1 (07-02-2017)

Identifiers

Cite

Caroline Castera-Ducros, Lucie Paloque, Pierre Verhaeghe, Magali Casanova, Christophe Cantelli, et al.. Targeting the human parasite Leishmania donovani: Discovery of a new promising anti-infectious pharmacophore in 3-nitroimidazo[1,2-a]pyridine series. Bioorganic and Medicinal Chemistry, 2013, 21 (22), pp.7155--7164. ⟨10.1016/j.bmc.2013.09.002⟩. ⟨hal-01460446⟩
197 View
0 Download

Altmetric

Share

Gmail Facebook Twitter LinkedIn More