2-Pyridinyl-3-(4-methylsulfonyl)phenylpyridines: selective and orally active cyclooxygenase-2 inhibitors |
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| Authors: | RW Friesen C Brideau CC Chan S Charleson D Deschênes D Dubé D Ethier R Fortin JY Gauthier Y Girard R Gordon GM Greig D Riendeau C Savoie Z Wang E Wong D Visco LJ Xu RN Young |
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| Affiliation: | Merck Frosst Centre for Therapeutic Research, Pointe Claire-Dorval, Québec, Canada. |
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| 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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