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.

引用

页码：2315 / 2320

页数：6

共 31 条

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