SYNTHESIS AND HIV-1 REVERSE-TRANSCRIPTASE INHIBITION PROPERTIES OF 2 NEW METHYLENEPHOSPHONATE ANALOGS OF 3'-AZIDO-3'-DEOXYTHYMIDINE-5'-TRIPHOSPHATE

被引：12
|
作者：
LABATAILLE, P [1 ]
PELICANO, H [1 ]
MAURY, G [1 ]
IMBACH, JL [1 ]
GOSSELIN, G [1 ]
机构：
[1] UNIV MONTPELLIER 2,CHIM BIOORGAN LAB,CNRS,URA 488,F-34095 MONTPELLIER 5,FRANCE
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1995年 / 5卷 / 20期
关键词：
D O I：
10.1016/0960-894X(95)00401-E
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Two new 5'-phosphorylated derivatives of 3'-azido-3'-deoxythymidine (AZT), namely alpha,beta;beta,gamma-bis (methylene) AZT-5'-triphosphate (1) under bar and alpha,beta-propylene AZT 5'-diphosphate (2) under bar, were synthesized. When evaluated for their inhibitory effects on human immunodeficiency virus (HIV) reverse transcriptase, these compounds were about 1000-fold less active than AZT-5'-triphosphate (AZTTP) as competitive inhibitors of this enzyme.
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收藏
页码：2315 / 2320
页数：6
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