期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 19, 期 2, 页码 502-507出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.11.030
关键词
Calpain inhibitor; Stroke; 4-Aryl-4-oxobutanoic acid; Ketoamide; Chromone
资金
- Korean Ministry of Commerce, Industry and Energy [10027898-2007-22]
- Seoul Research and Business Development Program [10524]
The involvement of mu-calpain in neurological disorders, such as stroke and Alzheimer's disease has attracted considerable interest in the use of calpain inhibitors as therapeutic agents. 4-Aryl-4-oxobutanoic acid amide derivatives 4 were designed as acyclic variants of mu-calpain inhibitory chromone and quinolinone derivatives. Of the compounds synthesized, 4c-2, which possesses a 2-methoxymethoxy group at the phenyl ring and a primary amide at the warhead region most potently inhibited mu-calpain (IC50 = 0.34 mu M). Our findings suggest that the 4-aryl-4-oxobutanoic acid amide derivatives should be considered as a new family of mu-calpain inhibitors. (C) 2008 Elsevier Ltd. All rights reserved.
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