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

BJ Al-Hourani, SK Sharma, M Suresh…

Index: Al-Hourani, Baker Jawabrah; Sharma, Sai Kiran; Suresh, Mavanur; Wuest, Frank Bioorganic and Medicinal Chemistry Letters, 2012 , vol. 22, # 6 p. 2235 - 2238

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Citation Number: 23

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 ...