Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors

A series of novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors was prepared via treatment of various diaryl amides with tetrachlorosilane/sodium azide. All compounds were tested in cyclooxygenase (COX) assays in vitro to determine COX-1 and COX-2 inhibitory potency and selectivity. Tetrazoles contained a methylsulfonyl or sulfonamide group as COX-2 pharmacophore displayed only low inhibitory potency towards COX-2. Most potent compounds showed IC50 values of 6 and 7 μM for COX-2. All compounds showed IC50 values greater 100 μM for COX-1 inhibition.

A series of novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors was prepared via treatment of various diaryl amides with tetrachlorosilane/sodium azide. All tetrazoles displayed only low inhibitory potency towards COX-2. Most potent compounds of the series displayed IC50 values of 6 and 7 μM for COX-2. All compounds showed IC50 values greater 100 μM for COX-1 inhibition.Figure optionsDownload as PowerPoint slide