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
  • 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.