2. Academic Validation
  3. 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

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

  • Bioorg Med Chem Lett. 2004 Apr 5;14(7):1683-8. doi: 10.1016/j.bmcl.2004.01.053.
Sunil Kumar Singh 1,  Saibaba Vobbalareddy,  Samala Shivaramakrishna,  A Krishnamraju,  Shaikh Abdul Rajjak,  Seshagiri Rao Casturi,  Vangoori Akhila,  Yeleswarapu Koteswar Rao
Affiliations

Affiliation

  • 1 Discovery Chemistry, Discovery Research-Dr Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500 049, India. sunilkumarsingh@drredys.com
PMID: 15026050 DOI: 10.1016/j.bmcl.2004.01.053
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.

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