Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)

被引：94
|
作者：
Sparks, Steven M. [1 ]
Chen, Grace [2 ]
Collins, Jon L. [1 ]
Danger, Dana [1 ]
Dock, Steven T. [1 ]
Jayawickreme, Channa [2 ]
Jenkinson, Stephen [3 ]
Laudeman, Christopher [3 ]
Leesnitzer, M. Anthony [2 ]
Liang, Xi [1 ]
Maloney, Patrick [3 ]
McCoy, David C. [3 ]
Moncol, David [2 ]
Rash, Vincent [2 ]
Rimele, Thomas [2 ]
Vulimiri, Padmaja [2 ]
Way, James M. [1 ]
Ross, Sean [1 ]
机构：
[1] GlaxoSmithKline, Enteroendocrine Discovery Performance Unit, Res Triangle Pk, NC 27705 USA
[2] GlaxoSmithKline, Platform Technol & Sci, Res Triangle Pk, NC 27705 USA
[3] GlaxoSmithKline, Metab Ctr Excellence Drug Discovery, Res Triangle Pk, NC 27705 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2014年 / 24卷 / 14期
关键词：
Free fatty acid receptor 4; Free fatty acid receptor 4 agonist; Free fatty acid receptor 4 antagonist; FFA4; GPR120; GLUCAGON-LIKE PEPTIDE-1; GLUCOSE-METABOLISM; INSULIN-SECRETION; L-CELL; GPR120; EXPRESSION; RELEASE; POTENT; GLP-1; GPR40;
D O I：
10.1016/j.bmcl.2014.05.012
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein. (C) 2014 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3100 / 3103
页数：4
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