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

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

European journal of medicinal chemistry (2012-11-21)
Sophie Marhadour, Pascal Marchand, Fabrice Pagniez, Marc-Antoine Bazin, Carine Picot, Olivier Lozach, Sandrine Ruchaud, Maud Antoine, Laurent Meijer, Najma Rachidi, Patrice Le Pape
ANOTACE

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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Sigma-Aldrich
Imidazo[1,2-a]pyridine, 99%