Acyloxymethyl and 4-acyloxybenzyl diester prodrugs of phosphonoformate

被引：21

作者：

Briggs, AD

Camplo, M

Freeman, S

Lundstrom, J

Pring, BG

机构：

[1] UNIV MANCHESTER,DEPT PHARM,MANCHESTER M13 9PL,LANCS,ENGLAND

[2] ASTRA ARCUS AB,S-15185 SODERTALJE,SWEDEN

来源：

TETRAHEDRON | 1996年 / 52卷 / 47期

关键词：

D O I：

10.1016/0040-4020(96)00906-4

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Sodium pivaloyloxymethyl (pivaloyloxymethoxycarbonyl)phosphonate 4, sodium 4-acyloxybenzyl phenoxycarbonylphosphonates 14a-c and sodium 4-acyloxybenzyl benzyloxycarbonylphosphonates 15a,b have been prepared as bioreversible prodrugs of the antiviral phosphonoformate 1. Their hydrolyses, in vivo systemic bioavailability and antiviral activity are reported. Of the compounds evaluated 4 was the best prodrug. Copyright (C) 1996 Elsevier Science Ltd

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页码：14937 / 14950

页数：14

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