Potent tricyclic pyrazole tetrazole agonists of the nicotinic acid receptor (GPR109a)

被引：31

作者：

Boatman, P. Douglas ^{[1
]}

Schrader, Thomas O. ^{[1
]}

Kasem, Michelle ^{[1
]}

Johnson, Benjamin R. ^{[1
]}

Skinner, Philip J. ^{[1
]}

Jung, Jae-Kyu ^{[1
]}

Xu, Jerry ^{[1
]}

Cherrier, Martin C. ^{[1
]}

Webb, Peter J. ^{[1
]}

Semple, Graeme ^{[1
]}

Sage, Carleton R. ^{[1
]}

Knudsen, Jens ^{[1
]}

Chen, Ruoping ^{[2
]}

Taggart, Andrew K. ^{[3
]}

Carballo-Jane, Ester ^{[3
]}

Richman, Jeremy G. ^{[2
]}

机构：

[1] Arena Pharmaceut, Dept Med Chem, San Diego, CA 92121 USA

[2] Arena Pharmaceut, Dept Discovery Biol, San Diego, CA 92121 USA

[3] Merck Res Labs, Rahway, NJ USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 09期

关键词：

Niacin receptor; Free fatty acids; Vasodilation; Atherosclerosis; TERMINAL EPOXIDES; PROSTAGLANDIN D-2; LANGERHANS CELLS; NIACIN; MK-0354; DISEASE; HUMANS; DRUG; MICE;

D O I：

10.1016/j.bmcl.2010.03.062

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Tricyclic pyrazole tetrazoles which are potent partial agonists of the high affinity niacin receptor, GPR109a, have been discovered and optimized. One of these compounds has proven to be effective at lowering free fatty acids in vitro and in vivo. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：2797 / 2800

页数：4

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