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

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

Bioorganic & medicinal chemistry letters (2012-02-22)
Baker Jawabrah Al-Hourani, Sai Kiran Sharma, Mavanur Suresh, Frank Wuest
PMID22341941
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.