Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors
BJ Al-Hourani, SK Sharma, M Suresh… - Bioorganic & medicinal …, 2012 - Elsevier
Bioorganic & medicinal chemistry letters, 2012•Elsevier
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 7μM for COX-2. All …
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 7μM for COX-2. All …
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 7μM for COX-2. All compounds showed IC50 values greater 100μM for COX-1 inhibition.
Elsevier
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