An evaluation of a C-glucuronide as a liver targeting group: Conjugate of a glucocorticoid antagonist

被引：14

作者：

Sorensen, BK

Link, JT

von Geldern, T

Emery, M

Wang, JH

Hickman, B

Grynfarb, M

Goos-Nilsson, A

Carroll, S

机构：

[1] Abbott Labs, Metab Dis Res, Abbott Pk, IL 60064 USA

[2] Karo Bio AB Novum, SE-14157 Huddinge, Sweden

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2003年 / 13卷 / 14期

关键词：

D O I：

10.1016/S0960-894X(03)00431-1

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A beta-C-glucuronide conjugate of the glucocorticoid receptor antagonist, Mifepristone 1, was prepared which maintained binding affinity, had modest in vitro activity, and was metabolically more stable than the parent. Pharmacokinetic studies suggest that the conjugate is recognized by the liver like O-glucuronides and may undergo a portion of the enterohepatic recirculation loop. (C) 2003 Elsevier Science Ltd. All rights reserved.

引用

页码：2307 / 2310

页数：4

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