2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines:: Selective and orally active cyclooxygenase-2 inhibitors

被引：131

作者：

Friesen, RW ^{[1
]}

Brideau, C ^{[1
]}

Chan, CC ^{[1
]}

Charleson, S ^{[1
]}

Deschênes, D ^{[1
]}

Dubé, D ^{[1
]}

Ethier, D ^{[1
]}

Fortin, R ^{[1
]}

Gauthier, JY ^{[1
]}

Girard, Y ^{[1
]}

Gordon, R ^{[1
]}

Greig, GM ^{[1
]}

Riendeau, D ^{[1
]}

Savoie, C ^{[1
]}

Wang, ZY ^{[1
]}

Wong, E ^{[1
]}

Visco, D ^{[1
]}

Xu, LJ ^{[1
]}

Young, RN ^{[1
]}

机构：

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

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 19期

关键词：

D O I：

10.1016/S0960-894X(98)00499-5

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-I, and COX-2. Optimum COX-2 activity is observed by introduction of a substituent at C5 of the central pyridine. 5-Chloro-3-(4-methylsulfonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine 33 was identified as the optimum compound in this series. (C) 1998 Published by Elsevier Science Ltd. All rights reserved.

引用

页码：2777 / 2782

页数：6

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