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

Eur J Med Chem. 2011 May;46(5):1694-700. doi: 10.1016/j.ejmech.2011.02.021.

Vijay K Marrapu ¹, Monika Mittal, Rahul Shivahare, Suman Gupta, Kalpana Bhandari

Affiliations

Affiliation

1 Medicinal and Process Chemistry Division, Central Drug Research Institute, CSIR, Lucknow 226 001, India.

PMID: 21385661 DOI: 10.1016/j.ejmech.2011.02.021

Abstract

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 μM while 11 compounds exhibited IC50 in the range of 3.04-9.39 μM against amastigotes. Compound 4, a 3-chlorobenzyloxy furanyl imidazole emerged as the most active compound in the series with IC50 value of 3.04 μM and SI value of 19.80, and was several folds more potent than the reference drugs miltefosine and miconazole.

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