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

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.

Graphical abstractThe easy access to 30 derivatives and the corresponding antiparasitic activities were described.Figure optionsDownload full-size imageDownload as PowerPoint slideHighlights► 2,3-Diarylimidazo[1,2-a]pyridines exhibited good antileishmanial activities. ► The impact of compound lipophilicity on antiparasitic activities was investigated. ► LmCK1 was detected as possible molecular target.