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

Journal Article

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

Bioorganic and Medicinal Chemistry Letters (2004) 14(7) 1683-1688

DOI: 10.1016/j.bmcl.2004.01.053

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Abstract

The effect of methanesulfonamide (MeSO2NH) group on COX-2 inhibitory activity of 1,5-diarylpyrazole is described. While this group being at position-4 of the N1-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 IC50 as low as 30 nM. © 2004 Elsevier Ltd. All rights reserved.

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Singh, S. K., Vobbalareddy, S., Shivaramakrishna, S., Krishnamraju, A., Rajjak, S. A., Casturi, S. R., … Rao, Y. K. (2004). 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. Bioorganic and Medicinal Chemistry Letters, 14(7), 1683–1688. https://doi.org/10.1016/j.bmcl.2004.01.053

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

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