Synthesis and biological evaluation of 3-heteroarizoxy-4-phenyl-2(5H)-furanones as selective COX-2 inhibitors

被引：35

作者：

Lau, CK ^{[1
]}

Brideau, C ^{[1
]}

Chan, CC ^{[1
]}

Charleson, S ^{[1
]}

Cromlish, WA ^{[1
]}

Ethier, D ^{[1
]}

Gauthier, JY ^{[1
]}

Gordon, R ^{[1
]}

Guay, J ^{[1
]}

Kargman, S ^{[1
]}

Li, CS ^{[1
]}

Prasit, P ^{[1
]}

Riendeau, D ^{[1
]}

Thérien, M ^{[1
]}

Visco, DM ^{[1
]}

Xu, LJ ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 22期

关键词：

D O I：

10.1016/S0960-894X(99)00560-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 3-heteroaryloxy-4-phenyl-2-(5H)-furanones were prepared and evaluated for their potency and selectivity as COX-2 inhibitors. This led to the identification of L-778,736 as a potent, orally active and selective inhibitor of the COX-2 enzyme. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：3187 / 3192

页数：6

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