Pyridopyrimidine based cannabinoid-1 receptor inverse agonists: Synthesis and biological evaluation

被引：20

作者：

Debenham, John S. ^{[1
]}

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

Wang, Junying ^{[1
]}

Tong, Xinchun ^{[1
]}

Lao, Julie ^{[2
]}

Fong, Tung M. ^{[2
]}

Schaeffer, Marie-Therese ^{[2
]}

Xiao, Jing Chen ^{[2
]}

Huang, Cathy C. R. -R. ^{[2
]}

Shen, Chun-Pyn ^{[2
]}

Stribling, D. Sloan ^{[3
]}

Shearman, Lauren P. ^{[3
]}

Strack, Alison M. ^{[3
]}

MacIntyre, D. Euan ^{[3
]}

Hale, Jeffrey J. ^{[1
]}

Walsh, Thomas F. ^{[1
]}

机构：

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

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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2009年 / 19卷 / 09期

关键词：

Cannabinoid; CB1; Inverse agonist; Pyridopyrimidine; Obesity; CB1; 5,6-DIARYLPYRIDINES;

D O I：

10.1016/j.bmcl.2009.03.005

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis, SAR and binding affinities are described for cannabinoid-1 receptor (CB1R) specific inverse agonists based on pyridopyrimidine and heterotricyclic scaffolds. Food intake and pharmacokinetic evaluation of several of these compounds indicate that they are effective orally active modulators of CB1R. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：2591 / 2594

页数：4

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