Synthesis and anti-retroviral activity of <i>O</i>,<i>O</i>′-<i>bis</i>(3′-azido-2′,3′-dideoxythymidin-5′-yl) phosphoramidate derivatives

作     者：Kers, I Stawinski, J Girardet, JL Imbach, JL Périgaud, C Gosselin, G Aubertin, AM 

作者机构：Univ Stockholm Arrhenius Lab Dept Organ Chem S-10691 Stockholm Sweden Univ Montpellier 2 Chim Bioorgan Lab CNRS UMR 5625 F-34095 Montpellier 5 France Fac Med Strasbourg Inst Virol INSERM U74 F-67000 Strasbourg France 

出 版 物：《NUCLEOSIDES & NUCLEOTIDES》 (核苷、核苷酸与核酸)

年 卷 期：1999年第18卷第10期

页      面：2317-2325页

核心收录：

学科分类：0710[理学-生物学] 071010[理学-生物化学与分子生物学] 07[理学] 

基　　金：Stiftelsen för Strategisk Forskning, SSF Agence Nationale de Recherches sur le Sida et les Hépatites Virales, ANRS Vetenskapsrådet, VR 

主　　题：酰胺类/化学 抗HIV药/化学合成 抗HIV药/化学 抗HIV药/药理学 细胞 培养的 HIV-1/药物作用 核苷类/化学合成 核苷类/化学 核苷类/药理学 磷酸类/化学 药物前体/化学合成 药物前体/化学 药物前体/药理学 病毒复制/药物作用 齐多夫定/类似物和衍生物 人类 

摘      要：A simple and efficient protocol for the preparation of various symmetrical dinucleoside phosphoramidates derived from AZT, is presented. It consists of the phosphonylation of AZT with phosphonic acid in the presence of DCC to produce the symmetrical H-phosphonate diester, followed by its oxidative conversion to various phosphoramidate analogues. The synthesized compounds were evaluated for their anti-HIV activity in different cell cultures.