Synthesis and activity of 4,5-diarylimidazoles as human CB1 receptor inverse agonists

被引：59

作者：

Plummer, CW

Finke, PE

Mills, SG

Wang, JY

Tong, XC

Doss, GA

Fong, TM

Lao, JZ

Schaeffer, MT

Chen, J

Shen, CP

Stribling, DS

Shearman, LP

Strack, AM

Van der Ploeg, LHT

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 Dis, Rahway, NJ 07065 USA

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 05期

关键词：

imidazole; obesity; CB1 inverse agonist; cannabinoid;

D O I：

10.1016/j.bmcl.2004.12.078

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-activity relationship studies directed toward the optimization of 4,5-diarylimidazole-2-carboxamide analogs as human CBI receptor inverse agonists resulted in the discovery of the two amide derivatives 24a and b (hCB1 IC50 = 6.1 and 4.0 nM) which also demonstrated efficacy in overnight feeding studies in the rat for reduction in both food intake and overall body weight. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：1441 / 1446

页数：6

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