Sar in the alkoxy lactone series:: The discovery of DFP, a potent and orally active COX-2 inhibitor

被引：49

作者：

Leblanc, Y

Roy, P

Boyce, S

Brideau, C

Chan, CC

Charleson, S

Gordon, R

Grimm, E

Guay, J

Léger, S

Li, CS

Riendeau, D

Visco, D

Wang, Z

Webb, J

Xu, LJ

Prasit, P

机构：

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

[2] Merck Res Labs, Harlow, Essex, England

[3] Merck Res Labs, Rahway, NJ USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1999年 / 9卷 / 15期

关键词：

D O I：

10.1016/S0960-894X(99)00365-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Extensive SAR has been established in the alkoxy lactone series and this has lead to the discovery of DFP (5,5-dimethyl-3-(2-propoxy)-4-methanesulfonylphenyl)-2-(5H)-furanone), a potent COX-2 inhibitor exhibiting in vivo efficacy in all models studied. (C) 1999 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：2207 / 2212

页数：6

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