Synthesis and biological evaluation of 2,3-diarylimidazo[1,2-a]pyridines as antileishmanial agents

Eur J Med Chem. 2012 Dec:58:543-56. doi: 10.1016/j.ejmech.2012.10.048.

Sophie Marhadour ¹, Pascal Marchand, Fabrice Pagniez, Marc-Antoine Bazin, Carine Picot, Olivier Lozach, Sandrine Ruchaud, Maud Antoine, Laurent Meijer, Najma Rachidi, Patrice Le Pape

Affiliations

Affiliation

1 Université de Nantes, Nantes Atlantique Universités, Laboratoire de Chimie Thérapeutique, Cibles et Médicaments des Infections et du Cancer, IICiMed UPRES EA 1155, UFR des Sciences Pharmaceutiques et Biologiques, 1 rue Gaston Veil, 44035 Nantes, France.

PMID: 23164660 DOI: 10.1016/j.ejmech.2012.10.048

Abstract

A novel series of 2,3-diarylimidazo[1,2-a]pyridines was synthesized and evaluated for their antileishmanial activities. Four derivatives exhibited good activity against the promastigote and intracellular amastigote stages of Leishmania major, coupled with a low cytotoxicity against the HeLa human cell line. The impact of compound lipophilicity on antiparasitic activities was investigated by Log D comparison. Although LmCK1 could be the parasitic target for three compounds (13, 18, 21), the inhibition of another target is under study to explain the antileishmanial effect of the most promising compounds.

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