Synthesis and biological evaluation of 2,3-diarylthiophenes as selective Cox-2 and Cox-1 inhibitors

Synthesis and biological evaluation of 2,3-diarylthiophenes as selective Cox-2 and Cox-1 inhibitors

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 relati...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters Vol. 5; no. 18; pp. 2123 - 2128
Main Authors: Leblanc, Yves, Gauthier, JacquesYves, Ethier, Diane, Guay, Jocelyne, Mancini, Joseph, Riendeau, Denis, Tagari, Philip, Vickers, Philip, Wong, Elizabeth, Prasit, Petpiboon
Format: Journal Article
Language:English
Published: Elsevier Ltd 21-09-1995
Online Access:Get full text
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Summary: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. Several 2,3-diarythiophene compounds were prepared and their activities against both cyclooxygenase isoforms were evaluated.
ISSN:0960-894X
1464-3405
DOI:10.1016/0960-894X(95)00359-2