Furo[2,3-b]pyridine-based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation. Part 1

被引：24

作者：

Debenham, John S. ^{[1
]}

Madsen-Duggan, Christina B. ^{[1
]}

Toupence, Richard B. ^{[1
]}

Walsh, Thomas F. ^{[1
]}

Wang, Junying ^{[1
]}

Tong, Xinchun ^{[1
]}

Kumar, Sanjeev ^{[2
]}

Lao, Julie ^{[3
]}

Fong, Tung M. ^{[3
]}

Xiao, Jing Chen ^{[3
]}

Huang, Cathy R-R. C. ^{[3
]}

Shen, Chun-Pyn ^{[3
]}

Feng, Yue ^{[3
]}

Marsh, Donald J. ^{[3
]}

Stribling, D. Sloan ^{[4
]}

Shearman, Lauren P. ^{[4
]}

Strack, Alison M. ^{[4
]}

Goulet, Mark T. ^{[1
]}

机构：

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

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

[3] Merck Res Labs, Dept Metab Disorders, Rahway, NJ 07065 USA

[4] Merck Res Labs, Dept Pharmacol, Rahway, NJ 07065 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 04期

关键词：

CB1R; Cannabinoid; Obesity; Inverse agonist; Furopyridine; BARIATRIC SURGERY; CB1; 5,6-DIARYLPYRIDINES; ANTAGONISTS; DISCOVERY; MORTALITY; OUTCOMES; OBESITY;

D O I：

10.1016/j.bmcl.2009.12.065

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis, SAR and binding affinities of cannabinoid-1 receptor (CB1R) inverse agonists based on furo[2,3-b]pyridine scaffolds are described. Food intake, mechanism specific efficacy, pharmacokinetic, and metabolic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：1448 / 1452

页数：5

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