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

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Abstract

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.

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