Discovery of 5-aryloxy-2,4-thiazolidinediones as potent GPR40 agonists

被引：50

作者：

Zhou, Changyou ^{[1
]}

Tang, Cheng ^{[1
]}

Chang, Eric ^{[1
]}

Ge, Min ^{[1
]}

Lin, Songnian ^{[1
]}

Cline, Eric ^{[1
]}

Tan, Carina P. ^{[1
]}

Feng, Yue ^{[1
]}

Zhou, Yun-Ping ^{[1
]}

Eiermann, George J. ^{[1
]}

Petrov, Aleksandr ^{[1
]}

Salituro, Gino ^{[1
]}

Meinke, Peter ^{[1
]}

Mosley, Ralph ^{[1
]}

Akiyama, Taro E. ^{[1
]}

Einstein, Monica ^{[1
]}

Kumar, Sanjeev ^{[1
]}

Berger, Joel ^{[1
]}

Howard, Andrew D. ^{[1
]}

Thornberry, Nancy ^{[1
]}

Mills, Sander G. ^{[1
]}

Yang, Lihu ^{[1
]}

机构：

[1] Merck Res Labs, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 03期

关键词：

GPR40; Agonist; 5-Aryloxy-2,4-thiazolidinediones; Diabetic; Hypoglycemia; GDIS; GSIS; SMALL-MOLECULE AGONISTS; INSULIN-SECRETION; FATTY-ACIDS; RECEPTOR; TARGET; ANTAGONISTS; MODULATORS; SAR;

D O I：

10.1016/j.bmcl.2009.10.052

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Systematic structure-activity relationship (SAR) studies of a screening lead led to the discovery of a series of thiazolidinediones (TZDs) as potent GPR40 agonists. Among them, compound C demonstrated an acute mechanism-based glucose-lowering in an intraperitoneal glucose tolerance test (IPGTT) in lean mice, while no effects were observed in GPR40 knock-out mice. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1298 / 1301

页数：4

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