SYNTHESIS, HYDROLYTIC BEHAVIOR, AND ANTI-HIV ACTIVITY OF SELECTED ACYLOXYALKYL ESTERS OF TRISODIUM PHOSPHONOFORMATE (FOSCARNET SODIUM)

被引：14

作者：

IYER, RP ^{[1
]}

BOAL, JH ^{[1
]}

PHILLIPS, LR ^{[1
]}

THAKKER, DR ^{[1
]}

EGAN, W ^{[1
]}

机构：

[1] US FDA,CTR BIOL EVALUAT & RES,BETHESDA,MD 20892

来源：

JOURNAL OF PHARMACEUTICAL SCIENCES | 1994年 / 83卷 / 09期

关键词：

D O I：

10.1002/jps.2600830916

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The synthesis and anti-HIV activity of selected (acyloxy)alkyl esters of trisodium phosphonoformate (foscarnet sodium) are described. The conversion of bis(trimethylsilyl) (alkoxycarbonyl)phosphonates 11a-d to the corresponding disilver salts 12a-d and their subsequent reaction with iodoalkyl acrylates 4a-c gave the desired bis(acyloxyalkyl) phosphonates 6-9(a-c). Of the analogs tested, only the dichlorophenyl analog 9a showed a dose-dependent inhibition of HIV activity in H9 cells. Using P-31-NMR, bioreversibility has been investigated in an attempt to rationalize these results.

引用

页码：1269 / 1273

页数：5

共 27 条

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