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

Authors
Nicoll-Griffith, DA Yergey, JA Trimble, LA Silva, JM Li, C Chauret, N Gauthier, JY Grimm, E Leger, S Roy, P Therien, M Wang, ZY Prasit, P Zamboni, R Young, RN Brideau, C Chan, CC Mancini, J Riendeau, D
Citation
Da. Nicoll-griffith et al., Synthesis, characterization, and activity of metabolites derived from the cyclooxygenase-2 inhibitor rofecoxib (MK-0966, Vioxx (TM)), BIOORG MED, 10(23), 2000, pp. 2683-2686
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
23
Year of publication
2000
Pages
2683 - 2686
Database
ISI
SICI code
0960-894X(200012)10:23<2683:SCAAOM>2.0.ZU;2-T
Abstract
Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx(TM)) were prep ared 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 rofe coxib inhibits COX-I nor contributes significantly to the inhibition of COX -2. (C) 2000 Elsevier Science Ltd. All rights reserved.