Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx™)

DA Nicoll-Griffith, JA Yergey, LA Trimble…

文献索引：Nicoll-Griffith, Deborah A.; Yergey, James A.; Trimble, Laird A.; Silva, Jose M.; Li, Chun; Chauret, Nathalie; Gauthier, Jacques Yves; Grimm, Erich; Leger, Serge; Roy, Patrick; Therien, Michel; Wang, Zhaoyin; Prasit, Peppi; Zamboni, Robert; Young, Robert N.; Brideau, Christine; Chan, Chi-Chung; Mancini, Joseph; Riendeau, Denis Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 23 p. 2683 - 2686

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被引用次数: 43

摘要

Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx™) were prepared by synthetic or biosynthetic methods. Metabolites include products of oxidation, glucuronidation, reduction and hydrolytic ring opening. Based on an in vitro whole blood assay, none of the known human metabolites of rofecoxib inhibits COX-1 nor contributes significantly to the inhibition of COX-2.