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
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
收藏
页码:2207 / 2212
页数:6
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