Bioorganic & Medicinal Chemistry Letters 2004-04-05

Methanesulfonamide group at position-4 of the C-5-phenyl ring of 1,5-diarylpyrazole affords a potent class of cyclooxygenase-2 (COX-2) inhibitors.

Sunil Kumar Singh, Saibaba Vobbalareddy, Samala Shivaramakrishna, A Krishnamraju, Shaikh Abdul Rajjak, Seshagiri Rao Casturi, Vangoori Akhila, Yeleswarapu Koteswar Rao

Index: Bioorg. Med. Chem. Lett. 14(7) , 1683-8, (2004)

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Abstract

The effect of methanesulfonamide (MeSO(2)NH) group on COX-2 inhibitory activity of 1,5-diarylpyrazole is described. While this group being at position-4 of the N(1)-phenyl ring was found to be ineffective, its installation at position-4 of the C-5 phenyl ring offered several potent and selective inhibitors of COX-2 with IC(50) as low as 30 nM.