Synthesis and evaluation of new furanyl and thiophenyl azoles as antileishmanial agents

A series of benzyloxy furanyl and benzyloxy thiophenyl azoles were synthesized and screened for their in vitro antileishmanial activity against Leishmania donovani. Among all, 16 compounds have shown more than 90% inhibition against promastigotes at 20 mu M while 11 compounds exhibited IC50 in the range of 3.04-9.39 mu M against amastigotes. Compound 4, a 3-chlorobenzyloxy furanyl imidazole emerged as the most active compound in the series with IC50 value of 3.04 mu M and SI value of 19.80, and was several folds more potent than the reference drugs miltefosine and miconazole. (C) 2011 Elsevier Masson SAS. All rights reserved.