Sugar-substituted 2-azetidinone cholesterol absorption inhibitors: Enhanced potency by modification of the sugar

被引：86

作者：

Vaccaro, WD ^{[1
]}

Davis, HR ^{[1
]}

机构：

[1] Schering Plough Res Inst, Kenilworth, NJ 07033 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1998年 / 8卷 / 03期

关键词：

D O I：

10.1016/S0960-894X(98)00008-0

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

A glucuronide conjugate of the potent 2-azetidinone cholesterol absorption inhibitor Sch 58235 was synthesized to confirm the structure of a metabolite isolated from in vivo sources. A series of 2-azetidinone glycosides was prepared via Schmidt trichloroimidate methodology. Enhanced cholesterol absorption inhibition was achieved by modification of the sugar moiety. (C) 1998 Elsevier Science Ltd. All rights reserved.

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页码：313 / 318

页数：6

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