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

Authors
LEBLANC Y GAUTHIER JY ETHIER D GUAY J MANCINI J RIENDEAU D TAGARI P VICKERS P WONG E PRASIT P
Citation
Y. Leblanc et al., SYNTHESIS AND BIOLOGICAL EVALUATION OF 2,3-DIARYLTHIOPHENES AS SELECTIVE COX-2 AND COX-1 INHIBITORS, Bioorganic & medicinal chemistry letters, 5(18), 1995, pp. 2123-2128
Citations number
16
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
5
Issue
18
Year of publication
1995
Pages
2123 - 2128
Database
ISI
SICI code
0960-894X(1995)5:18<2123:SABEO2>2.0.ZU;2-2
Abstract
A series of 2,3-diarylthiophene compounds was prepared and their biolo gical activities were evaluated against human Cox-1 and Cox-2 enzymes. It appears that the methylsulfone group is essential for both the act ivity and selectivity for the Cox-2 enzyme. Removal of the methylsulfo ne group gave relatively selective Cox-1 inhibitors.