期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 103, 期 -, 页码 381-395出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.09.002
关键词
Antileishmanial activity; Imidazo[1,2-a]pyrazines; Direct arylation; Casein kinase 1
资金
- Canceropole Grand Ouest - Line Valorisation des produits de la mer
A series of original 2-phenyl-3-(pyridin-4-yl)imidazo[1,2-a]pyrazines and the 3-iodo precursors, bearing a polar moiety at the C-8 position, was synthesized and evaluated for their antileishmanial activities. Two derivatives exhibited very good activity against the promastigote and the amastigote forms of Leishmania major in the micromolar to submicromolar ranges, coupled with a low cytotoxicity against macrophages and 3T3 mouse fibroblast cells. Through LmCK1 inhibition assay, investigations of the putative molecular target of these promising antileishmanial compounds will be discussed. (C) 2015 Elsevier Masson SAS. All rights reserved.
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