Synthesis and evaluation of some novel phosphoramidate derivatives of 3 '-azido-3 '-deoxythymidine (AZT) as anti-HIV compounds

被引：63

作者：

McGuigan, C. ^{[1
]}

Devine, K. G. ^{[1
]}

O'Connor, T. J. ^{[2
]}

Galpin, S. A. ^{[2
]}

Jeffries, D. J. ^{[2
]}

Kinchington, D. ^{[2
]}

机构：

[1] Univ Coll London, Dept Chem, 20 Gordon St, London WC1H 0AJ, England

[2] St Marys Hosp, Med Sch, Dept Med Microbiol, Div Virol, London W2 1PG, England

来源：

ANTIVIRAL CHEMISTRY & CHEMOTHERAPY | 1990年 / 1卷 / 02期

基金：

英国医学研究理事会;

关键词：

D O I：

10.1177/095632029000100205

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：

A series of monophosphate triester derivatives of 3'-azido-3'-deoxythymidine (AZT), designed as membrane-soluble pro-drugs of the nucleotide (AZTMP), have been tested for activity against the human immunodeficiency virus (HIV-1). It has been found that when carboxyl-protected, amino-linked amino acids, and alkyl chains, are asymmetrically substituted on the 5'-phosphate a significant antiviral effect is observed. Moreover, the activity of the compounds is profoundly dependent on the structure of the phosphate moiety, and in particular on the nature of the amino acid.

引用

页码：107 / 113

页数：7

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