DIDEOXYNUCLEOSIDES AS POTENTIAL ANTI-AIDS DRUGS

介绍了一种合成具有水解性的双脱氧核素的方法。 被认为有潜在用途的抗艾滋病毒药物，一直以来 延伸到各种修饰的嘌呤和嘧啶碱。2‘-氟代 Ara构型中的取代基保护这些化合物 化学降解和酶降解。一些新化合物 人工合成的药物似乎起到了“前药”的作用，需要 腺苷脱氨酶来揭示它们的生物活性。 报道了一种合成含氟双脱氧核苷的新方法. 发展起来的。它极大地促进了这一过程，因为一个关键的还原 现在在缩合反应之前执行该步骤。这种反应是 只用于生产许多化合物一次，而不是每次 制备了一种新的化合物。 一系列双脱氧寡糖核苷正在被开发为潜在的 抗艾滋病毒药物。这些化合物被设计为部分结构的 抗生素oxetanocin的扩环类似物。

The methodology for the synthesis of hydrolytically stable dideoxy nucleo- sides, considered to be of potential use as anti-HIV agents, has been extended to various modified purine and pyrimidine bases. The 2'-fluoro substituent in the ara-configuration protects these compounds against chemical as well as enzymatic degradation. Some of the new compounds synthesized appear to function as "prodrugs" which require the action of adenosine deaminase to uncover their biological activity. A new synthetic approach toward fluorine-containing dideoxynucleosides was developed. It greatly facilitates the process since a critical reductive step is now performed before the condensation reaction. This reaction is used only once for the production of many compounds, rather than every time a new compound is prepared. A series of dideoxyapiose nucleosides is being developed as potential anti-HIV agents. These compounds were designed as partial structures of the ring expanded analogue of the antibiotic oxetanocin.