期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 46, 期 5, 页码 1694-1700出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2011.02.021
关键词
Antileishmanial; Miconazole; Azoles; Sterol biosynthesis inhibitors (SBIs)
资金
- Council of Scientific and Industrial Research (India)
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.
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