3-[4-(methylsulfonyl) phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone as a potent and orally active cyclooxygenase-2 selective inhibitor: Synthesis and biological …

SP Khanapure, ME Augustyniak, RA Earl…

文献索引：Khanapure, Subhash P.; Augustyniak, Michael E.; Earl, Richard A.; Garvey, David S.; Letts, L. Gordon; Martino, Allison M.; Murty, Madhavi G.; Schwalb, David J.; Shumway, Matthew J.; Trocha, Andrzej M.; Young, Delano V.; Zemtseva, Irina S.; Janero, David R. Journal of Medicinal Chemistry, 2005 , vol. 48, # 11 p. 3930 - 3934

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被引用次数: 10

摘要

Incorporation of a spacer group between the central scaffold and the aryl ring resulted in a new cyclooxygenase-2 (COX-2) selective inhibitor core structure, 3-[4-(methylsulfonyl) phenyl]-5-(trifluoromethyl)(2-pyridyl) phenyl ketone (20), with COX-2 IC50= 0.25 μM and COX-1 IC50= 14 μM (human whole blood assay). Compound 20 was orally active in the rat air pouch model of inflammation, inhibiting white blood cell infiltration and COX-2-derived ...