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

…, S Charleson, D Deschênes, D Dubé, D Ethier…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 19 p. 2777 - 2782

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被引用次数: 132

摘要

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.