Skip to Main content Skip to Navigation
Journal articles

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

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
Document type :
Journal articles
Complete list of metadatas

https://hal-amu.archives-ouvertes.fr/hal-01460446
Contributor : Didier Gigmes <>
Submitted on : Tuesday, February 7, 2017 - 4:42:02 PM
Last modification on : Wednesday, August 19, 2020 - 12:08:19 PM

Identifiers

Collections

Citation

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, Elsevier, 2013, 21 (22), pp.7155--7164. ⟨10.1016/j.bmc.2013.09.002⟩. ⟨hal-01460446⟩

Share

Metrics

Record views

294