3,4-diaryl-5-hydroxyfuranones:: Highly selective inhibitors of cyclooxygenase-2 with aqueous solubility

被引:33
作者
Black, WC [1 ]
Brideau, C [1 ]
Chan, CC [1 ]
Charleson, S [1 ]
Cromlish, W [1 ]
Gordon, R [1 ]
Grimm, EL [1 ]
Hughes, G [1 ]
Leger, S [1 ]
Li, CS [1 ]
Riendeau, D [1 ]
Thérien, M [1 ]
Wang, ZY [1 ]
Xu, LJ [1 ]
Prasit, P [1 ]
机构
[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada
关键词
D O I
10.1016/S0960-894X(03)00046-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The introduction of a hydroxyl group into the 5-position of the diaryl furanone system provides highly selective inhibitors of cyclooxygenase-2. These molecules can be converted into their sodium salts which are water soluble, facilitating intravenous formulation. These salts show excellent potency in rat models of pain, fever and inflammation. (C) 2003 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:1195 / 1198
页数:4
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