期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 16, 期 7, 页码 1840-1845出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2006.01.007
关键词
GPR40; GPR40 agonists; fatty acid receptor; type 2 diabetes; GPCR agonist; G-protein coupled receptor agonist; asymmetric cyclopropanation
The first report on the identification and structure-activity relationships of a novel series of GPR40 agonists based on a 3(4-{[N-alkyl]amino phenyl)propanoic acid template is described. Structural modifications to the original screening hit yielded compounds with a 100-fold increase in potency at the human GPR40 receptor and pEC(50)s in the low nanomolar range. The carboxylic acid moiety is not critical for activity but typically elicits an agonistic response higher than those observed with carboxamide replacements. These compounds may prove useful in unraveling the therapeutic potential of this receptor for the treatment of Type 2 diabetes. (C) 2006 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据