Application of the ''trimethyl lock'' to ganciclovir, a pro-prodrug with increased oral bioavailability

被引：16

作者：

Dillon, MP

Cai, HY

Maag, H

机构：

[1] Chemical Research and Development, Syntex Discovery Research, Palo Alto, CA 94304

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1996年 / 6卷 / 14期

关键词：

D O I：

10.1016/0960-894X(96)00294-6

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and oral bioavailability of two potential prodrugs of Ganciclovir (1) based on the ''trimethyl lock'' is described, The mono-3-(2'-Acetoxy-4'6'-dimethylphenyl)-3,3-dimethylpropanoic ester (2) showed a four-fold increase in oral bioavailability over the parent drug in rats. Copyright (C) 1996 Elsevier Science Ltd

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页码：1653 / 1656

页数：4

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