Structure-activity relationship studies on 2-heteroaryl-4-arylimidazoles NPY5 receptor antagonists

被引：31

作者：

Elliott, RL ^{[1
]}

Oliver, RM

LaFlamme, JA

Gillaspy, ML

Hammond, M

Hank, RF

Maurer, TS

Baker, DL

DaSilva-Jardine, PA

Stevenson, RW

Mack, CM

Cassella, JV

机构：

[1] Pfizer Global Res & Dev, Dept Cardiovasc & Metab Dis, Groton, CT 06340 USA

[2] Neurogen Corp, Branford, CT 06405 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 20期

关键词：

D O I：

10.1016/S0960-894X(03)00747-9

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2-heteroaryl-4-arylimidazoles with potent in vitro activity at the NPY5 receptor was developed. Introduction of electron-withdrawing groups on the 4-aryl ring led to a significant improvement of in vitro potency. Several analogues from this series had anorectic activity in rodent feeding models, but were also found to have undesired behavioral effects in spontaneous locomotor activity. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：3593 / 3596

页数：4

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