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

被引：38

作者：

Nicoll-Griffith, DA ^{[1
]}

Yergey, JA ^{[1
]}

Trimble, LA ^{[1
]}

Silva, JM ^{[1
]}

Li, C ^{[1
]}

Chauret, N ^{[1
]}

Gauthier, JY ^{[1
]}

Grimm, E ^{[1
]}

Léger, S ^{[1
]}

Roy, P ^{[1
]}

Thérien, M ^{[1
]}

Wang, ZY ^{[1
]}

Prasit, P ^{[1
]}

Zamboni, R ^{[1
]}

Young, RN ^{[1
]}

Brideau, C ^{[1
]}

Chan, CC ^{[1
]}

Mancini, J ^{[1
]}

Riendeau, D ^{[1
]}

机构：

[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2000年 / 10卷 / 23期

关键词：

D O I：

10.1016/S0960-894X(00)00538-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Metabolites of the COX-2 inhibitor rofecoxib (MK-0966, Vioxx(TM)) 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-I nor contributes significantly to the inhibition of COX-2. (C) 2000 Elsevier Science Ltd. All rights reserved.

引用

页码：2683 / 2686

页数：4

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