Synthesis, biological activity and decomposition studies of amino acid phosphomonoester amidates of acyclovir

被引：15

作者：

Abraham, TW

McIntee, EJ

Iyer, VV

Schinazi, RF

Wagner, CR

机构：

[1] UNIV MINNESOTA, COLL PHARM, DEPT MED CHEM, MINNEAPOLIS, MN 55455 USA

[2] EMORY UNIV, SCH MED, GEORGIA VA RES CTR AIDS & HIV INFECT, DEPT PEDIAT, DECATUR, GA 30033 USA

来源：

NUCLEOSIDES NUCLEOTIDES & NUCLEIC ACIDS | 1997年 / 16卷 / 10-11期

基金：

美国国家卫生研究院;

关键词：

D O I：

10.1080/07328319708002557

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

Highly stable and water soluble amino acid phosphomonoester amidates of acyclovir (ACV) were synthesized and shown to function predominantly as prodrugs of ACV and not acyclovir monophosphate (ACV-MP) with activities within two fold of the amino acid prodrug of ACV, valaciclovir (VACV). Metabolism studies revealed that incubation of cell-free extracts of Vero cells with the L-leucine phosphomonoester amidate of ACV (3c), resulted in a burst of ACV-MP production followed by the rapid generation of ACV.

引用

收藏

页码：2079 / 2092

页数：14

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