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

Caroline Castera-Ducros; Lucie Paloque; Pierre Verhaeghe; Magali Casanova; Christophe Cantelli; Sébastien Hutter; Floriane Tanguy; Michèle Laget; Vincent Remusat; Anita Cohen; Maxime D. Crozet; Pascal Rathelot; Nadine Azas; Patrice Vanelle

doi:10.1016/j.bmc.2013.09.002

Journal articles

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

Caroline Castera-Ducros Lucie Paloque ^{1, 2} Pierre Verhaeghe ² Magali Casanova ³ Christophe Cantelli Sébastien Hutter ³ Floriane Tanguy Michèle Laget ³ Vincent Remusat ⁴ Anita Cohen ³ Maxime D. Crozet ⁵ Pascal Rathelot ^{4, 6} Nadine Azas ³ Patrice Vanelle ⁴

1 UT3 - Université Toulouse III - Paul Sabatier

2 LCC - Laboratoire de chimie de coordination

3 IP-TPT - Infections Parasitaires : Transmission, Physiopathologie et Thérapeutiques

4 ICR - Institut de Chimie Radicalaire

5 CBRL - Chimie, biologie et radicaux libres - UMR 6517

6 APHM - Assistance Publique - Hôpitaux de Marseille

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

Domain :

Chemical Sciences

Life Sciences [q-bio] / Microbiology and Parasitology / Parasitology

Chemical Sciences / Medicinal Chemistry

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

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

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