期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 13, 页码 2949-2953出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.04.065
关键词
GPR40; Agonist; Diabetes; Insulin secretagogue; Glucose lowering
The G protein-coupled receptor 40 (GPR40) mediates enhancement of glucose-stimulated insulin secretion in pancreatic 0 cells. The GPR40 agonist has been attracting attention as a novel insulin secretagogue with glucose dependency for the treatment of type 2 diabetes. The optimization study of compound 1 led to a potent and bioavailable GPR40 agonist 24, which showed insulin secretion and glucose lowering effects in rat OGTT. Compound 24 is a potential lead compound for a novel insulin secretagogue with a low risk of hypoglycemia. (C) 2014 Elsevier Ltd. All rights reserved.
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