2-pyridinyl-3(4-methylsulfonyl)phenylpyridines: Selective and orally active cyclooxygenase-2 inhibitors
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.
Friesen, Richard W.,Brideau, Christine,Chan, Chi Chung,Charleson, Stella,Deschenes, Denis,Dube, Daniel,Ethier, Diane,Fortin, Rejean,Gauthier, Jacques Yves,Girard, Yves,Gordon, Robert,Greig, Gillian M.,Riendeau, Denis,Savoie, Chantai,Wang, Zhaoyin,Wong, Elizabeth,Visco, Denise,Xu, Li Jing,Young, Robert N.