CHARACTERIZATION OF THE IN-VITRO OXIDATIVE METABOLITES OF THE COX-2 SELECTIVE INHIBITOR L-766,112

Authors
TRIMBLE LA CHAURET N SILVA JM NICOLLGRIFFITH DA LI CS YERGEY JA
Citation
La. Trimble et al., CHARACTERIZATION OF THE IN-VITRO OXIDATIVE METABOLITES OF THE COX-2 SELECTIVE INHIBITOR L-766,112, Bioorganic & medicinal chemistry letters, 7(1), 1997, pp. 53-56
Citations number
11
Categorie Soggetti
Chemistry Inorganic & Nuclear","Chemistry Medicinal
Journal title
Bioorganic & medicinal chemistry letters → ACNP
ISSN journal
0960894X
Volume
7
Issue
1
Year of publication
1997
Pages
53 - 56
Database
ISI
SICI code
0960-894X(1997)7:1<53:COTIOM>2.0.ZU;2-0
Abstract
L-766,112 (1), a potent and selective inhibitor of human COX-2, was in cubated with rat and rhesus monkey hepatic microsomal fractions under oxidative conditions to generate a metabolite identified as the thioph ene S-oxide. This oxide was trapped with glutathione to give a conjuga te in which GSH added to the 3 position. The metabolites, also identif ied in rat hepatocyte incubations, were characterized by UV, NMR, and CF-LSIMS. Copyright (C) 1996 Elsevier Science Ltd