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ID: ALA1132833

Journal: Bioorg Med Chem Lett

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

Authors: Nicoll-Griffith DA, Yergey JA, Trimble LA, Silva JM, Li C, Chauret N, Gauthier JY, Grimm E, Léger S, Roy P, Thérien M, Wang Z, Prasit P, Zamboni R, Young RN, Brideau C, Chan CC, Mancini J, Riendeau D.

Abstract: 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.

CiteXplore: 11128651

DOI: 10.1016/s0960-894x(00)00538-2