3-Nitro-4-amino benzoic acids and 6-amino nicotinic acids are highly selective agonists of GPR109b

被引：22

作者：

Skinner, Philip J. ^{[1
]}

Cherrier, Martin C. ^{[1
]}

Webb, Peter J. ^{[1
]}

Sage, Carleton R. ^{[1
]}

Dang, Huong T. ^{[1
]}

Pride, Cameron C. ^{[1
]}

Chen, Ruoping ^{[1
]}

Tamura, Susan Y. ^{[1
]}

Richman, Jeremy G. ^{[1
]}

Connolly, Daniel T. ^{[1
]}

Semple, Graeme ^{[1
]}

机构：

[1] Arena Pharmaceut, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 23期

关键词：

D O I：

10.1016/j.bmcl.2007.09.058

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-nitro-4-substituted-aminobenzoic acids were prepared and found to act as potent and highly selective agonists of the orphan human GPCR GPR109b, a low affinity receptor for niacin. No activity was observed at the closely homologous high affinity niacin receptor, GPR109a. A second series, comprising 6-amino-substituted nicotinic acids was, also prepared and several analogues showed comparable activity to the nitroaryl series. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：6619 / 6622

页数：4

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