期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 58, 期 -, 页码 543-556出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.10.048
关键词
Antileishmanial activity; 2,3-Diarylimidazo[1,2-a]pyridines; Direct arylation; Lipophilicity; Casein kinase 1
资金
- EEC [FP7 HEALTH-2007-2.3.4-1: LEISHDRUG]
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. (C) 2012 Elsevier Masson SAS. All rights reserved.
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