7-Hydroxynaphthalen-1-y1-urea and -amide antagonists of human vanilloid receptor 1

被引：22

作者：

McDonnell, ME

Zhang, SP

Nasser, N

Dubin, AE

Dax, SL

机构：

[1] Johnson & Johnson Pharmaceut Res & Dev, Spring House, PA 19477 USA

[2] Johnson & Johnson Pharmaceut Res & Dev, San Diego, CA 92121 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 02期

关键词：

D O I：

10.1016/j.bmcl.2003.09.090

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of structurally simple 7-hydroxynaphthalenyl ureas and amides were discovered to be potent ligands of human vanilloid receptor I (VR1). 1-(7-Hydroxynaphthaten-1-yl)-3-(4-trifluoromethylbenzyl)urea 5f exhibited nanomolar binding affinity (K-i = 1.0 nM) and upon capsaicin challenge, behaved as a potent functional antagonist (IC50 = 4 nM). The synthesis and structure-activity relationships (SARs) for the series are described. (C) 2003 Elsevier Ltd. All rights reserved.

引用

页码：531 / 534

页数：4

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