GPR109a agonists. Part 2: Pyrazole-acids as agonists of the human orphan G-protein coupled receptor GPR109a

被引：10

作者：

Imbriglio, Jason E. ^{[1
]}

Chang, Sookhee ^{[1
]}

Liang, Rui ^{[1
]}

Raghavan, Subharekha ^{[1
]}

Schmidt, Darby ^{[1
]}

Smenton, Abby ^{[1
]}

Tria, Scott ^{[1
]}

Schrader, Thomas O. ^{[4
]}

Jung, Jae-Kyu ^{[4
]}

Esser, Craig ^{[1
]}

Holt, Tom G. ^{[2
]}

Wolff, Michael S. ^{[2
]}

Taggart, Andrew K. P. ^{[3
]}

Cheng, Kang ^{[3
]}

Carballo-Jane, Ester ^{[3
]}

Waters, M. Gerard ^{[3
]}

Tata, James R. ^{[1
]}

Colletti, Steven L. ^{[1
]}

机构：

[1] Merck & Co Inc, Dept Med Chem, Merck Res Labs, Rahway, NJ 07065 USA

[2] Merck & Co Inc, Dept Drug Metab, Merck Res Labs, Rahway, NJ 07065 USA

[3] Merck & Co Inc, Dept Cardiovasc Dis, Merck Res Labs, Rahway, NJ 07065 USA

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 15期

关键词：

Niacin; GPR109a; Agonists; NICOTINIC-ACID; MOLECULAR-IDENTIFICATION;

D O I：

10.1016/j.bmcl.2010.06.041

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

5-Alkyl and aryl-pyrazole-acids have been identified as a new class of selective, small-molecule, agonists of the human orphan G-protein-coupled receptor GPR109a, a high affinity receptor for the HDL-raising drug nicotinic acid. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：4472 / 4474

页数：3

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