2. Academic Validation
  3. 2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors

2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors

  • Bioorg Med Chem Lett. 1998 Oct 6;8(19):2777-82. doi: 10.1016/s0960-894x(98)00499-5.
R W Friesen 1,  C Brideau,  C C Chan,  S Charleson,  D Deschênes,  D Dubé,  D Ethier,  R Fortin,  J Y Gauthier,  Y Girard,  R Gordon,  G M Greig,  D Riendeau,  C Savoie,  Z Wang,  E Wong,  D Visco,  L J Xu,  R N Young
Affiliations

Affiliation

  • 1 Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada.
PMID: 9873621 DOI: 10.1016/s0960-894x(98)00499-5
Abstract

A series of novel 2-pyridinyl-3-(4-methylsulfonyl)phenylpyridines has been synthesized and evaluated with respect to their ability to inhibit the isozymes of cyclooxygenase, COX-1, and COX-2. Optimum COX-2 activity is observed by introduction of a substituent at C5 of the central pyridine. 5- Chloro-3-(4-methylsulfonyl)phenyl-2-(2-methyl-5-pyridinyl)pyridine 33 was identified as the optimum compound in this series.

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