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Novel 5-substituted 1H-tetrazoles as cyclooxygenase-2 (COX-2) inhibitors
Baker Jawabrah Al-Hourani1, Sai Kiran Sharma, Mavanur Suresh
1Department of Oncology, University of Alberta, Edmonton, Alberta, Canada.
Abstract:
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 IC(50) values of 6 and 7 μM for COX-2. All compounds showed IC(50) values greater 100 μM for COX-1 inhibition.
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