Biarylimidazoles as inhibitors of microsomal prostaglandin E2 synthase-1

被引：30

作者：

Wu, Tom Y. H. ^{[1
]}

Juteau, Helene ^{[1
]}

Ducharme, Yves ^{[1
]}

Friesen, Richard W. ^{[1
]}

Guiral, Sebastien ^{[1
]}

Dufresne, Lynn ^{[1
]}

Poirier, Hugo ^{[1
]}

Salem, Myriam ^{[1
]}

Riendeau, Denis ^{[1
]}

Mancini, Joseph ^{[1
]}

Brideau, Christine ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Kirkland, PQ H9H 3L1, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 23期

关键词：

mPGES-1; Inhibitor; Biarylimidazole; PGE2; Inflammation; CYCLOOXYGENASE-2; MPGES-1; AGENTS; ASSAY;

D O I：

10.1016/j.bmcl.2010.09.129

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Microsomal prostaglandin E-2 synthase (mPGES-1) represents a potential target for novel analgesic and anti-inflammatory agents. High-throughput screening identified several leads of mPGES-1 inhibitors which were further optimized for potency and selectivity. A series of inhibitors bearing a biaryl imidazole scaffold exhibits excellent inhibition of PGE(2) production in enzymatic and cell-based assays. The synthesis of these molecules and their activities will be discussed. (C) 2010 Elsevier Ltd. All rights reserved.

引用

页码：6978 / 6982

页数：5

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