Substituted acyclic sulfonamides as human cannabinoid-1 receptor inverse agonists

被引：19

作者：

Armstrong, Helen E.

Galka, Amy

Lin, Linus S.

Lanza, Thomas J., Jr.

Jewell, James P.

Shah, Shrenik K.

Guthikonda, Ravi

Truong, Quang

Chang, Linda L.

Quaker, Grace

Colandrea, Vincent J.

Tong, Xinchun

Wang, Junying

Xu, Sherry

Fong, Tung M.

Shen, Chun-Pyn

Lao, Julie

Chen, Jing

Shearman, Lauren P.

Stribling, D. Sloan

Rosko, Kimberly

Strack, Alison

Ha, Sookhee

Van der Ploeg, Lex

Goulet, Mark T.

Hagmann, William K. ^{[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

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 08期

关键词：

cannabinoid; CB-1R; sulfonamide; obesity;

D O I：

10.1016/j.bmcl.2007.01.087

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Sulfonamide analogues of the potent CB1R inverse agonist taranabant were prepared and optimized for potency and selectivity for CB I R. They were variably more potent than the corresponding amide analogues. The most potent representative 22 had good pharmacokinetic and brain levels, but was modestly active in blocking CB1R agonist-mediated hypothermia. (c) 2007 Elsevier Ltd. All rights reserved.

引用

页码：2184 / 2187

页数：4

共 14 条

[1] CB1 cannabinoid receptor antagonists for treatment of obesity and prevention of comorbid metabolic disorders [J].