Solid-phase combinatorial approach for the optimization of soluble epoxide hydrolase inhibitors

被引：27

作者：

Hwang, Sung Hee

Morisseau, Christophe

Do, Zung

Hammock, Bruce D.

机构：

[1] Univ Calif Davis, Dept Entomol, Davis, CA 95616 USA

[2] Univ Calif Davis, Ctr Canc, Davis, CA 95616 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2006年 / 16卷 / 22期

关键词：

soluble epoxide hydrolase; urea; hypertension; anti-inflammation;

D O I：

10.1016/j.bmcl.2006.08.078

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A 192-member library of N,N'-disubstituted urea inhibitors was synthesized by a solid-phase method. The ureas were tested for their inhibitory activities against recombinant human soluble epoxide hydrolase. Simple carbocyclic or paralmeta-substituted phenyl groups showed inhibition potencies that were equal to or greater than adamantane-based sEH inhibitors, while the presence of bulky or ionizable groups close to the urea group dramatically decreased their activities. (c) 2006 Elsevier Ltd. All rights reserved.

引用

收藏

页码：5773 / 5777

页数：5

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