SYNTHESIS AND BIOLOGICAL EVALUATION OF 2,3-DIARYLTHIOPHENES AS SELECTIVE COX-2 AND COX-1 INHIBITORS

被引：65

作者：

LEBLANC, Y

GAUTHIER, JY

ETHIER, D

GUAY, J

MANCINI, J

RIENDEAU, D

TAGARI, P

VICKERS, P

WONG, E

PRASIT, P

机构：

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 18期

关键词：

D O I：

10.1016/0960-894X(95)00359-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A series of 2,3-diarylthiophene compounds was prepared and their biological activities were evaluated against human Cox-1 and Cox-2 enzymes. It appears that the methylsulfone group is essential for both the activity and selectivity for the Cox-2 enzyme. Removal of the methylsulfone group gave relatively selective Cox-1 inhibitors.

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页码：2123 / 2128

页数：6

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