2-hydroxymethyl-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl]-1-benzenesulfonamide (DRF-4367): an orally active COX-2 inhibitor identified through pharmacophoric modulation.

  title={2-hydroxymethyl-4-[5-(4-methoxyphenyl)-3-trifluoromethyl-1H-1-pyrazolyl]-1-benzenesulfonamide (DRF-4367): an orally active COX-2 inhibitor identified through pharmacophoric modulation.},
  author={S. Singh and Saibaba Vobbalareddy and Srinivasa Rao Kalleda and S. A. Rajjak and S. R. Casturi and S. Datla and R. Mamidi and R. Mullangi and Ravikanth Bhamidipati and R. Ramanujam and V. Akella and K. R. Yeleswarapu},
  journal={Organic & biomolecular chemistry},
  volume={2 17},
  • S. Singh, Saibaba Vobbalareddy, +9 authors K. R. Yeleswarapu
  • Published 2004
  • Chemistry, Medicine
  • Organic & biomolecular chemistry
  • Analogs of 1,5-diarylpyrazoles with a novel pharmacophore at N1 were designed, synthesized and evaluated for the in-vitro cyclooxygenase (COX-1/COX-2) inhibitory activity. The variations at/around position-4 of the C-5 phenyl ring in conjunction with a CF3 and CHF2 groups at C-3 exhibited a high degree of potency and selectivity index (SI) for COX-2 inhibition. The in-vivo evaluation of these potent compounds with a few earlier ones indicated the 4-OMe-phenyl analog and the 4-NHMe-phenyl analog… CONTINUE READING
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