Synthesis and cyclooxygenase-2 inhibiting property of 1, 5-diarylpyrazoles with substituted benzenesulfonamide moiety as pharmacophore: preparation of sodium salt …

…, A Vanguri, R Mullangi, NVS Rao Mamidi…

Index: Pal, Manojit; Madan, Manjula; Padakanti, Srinivas; Pattabiraman, Vijaya R.; Kalleda, Srinivas; Vanguri, Akhila; Mullangi, Ramesh; Mamidi, N. V. S. Rao; Casturi, Seshagiri R.; Malde, Alpeshkumar; Gopalakrishnan; Yeleswarapu, Koteswar R. Journal of Medicinal Chemistry, 2003 , vol. 46, # 19 p. 3975 - 3984

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Citation Number: 54

Abstract

A series of 1, 5-diarylpyrazoles having a substituted benzenesulfonamide moiety as pharmacophore was synthesized and evaluated for cyclooxygenase (COX-1/COX-2) inhibitory activities. Through SAR and molecular modeling, it was found that fluorine substitution on the benzenesulfonamide moiety along with an electron-donating group at the 4-position of the 5-aryl ring yielded selectivity as well as potency for COX-2 inhibition in ...