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无环异胞嘧啶和9-脱氮腺嘌呤C-核苷新型SATE衍生物的设计与合成。

Design and synthesis of novel SATE derivatives of acyclic isocytosine and 9-deazaadenine C-nucleosides.

作者信息

Liu Lian Jin, Hong Joon Hee

机构信息

College of Pharmacy, Chosun University, Kwangju, Republic of Korea.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2010 Mar;29(3):257-66. doi: 10.1080/15257771003745704.

Abstract

This article describes a very simple route for synthesizing novel lipophilic phosphate bis(t-bu-SATE) prodrugs of acyclic cyclobutylated C-nucleosides such as isocytosine 12 and 9-deazaadenine 19, which were prepared from 1,1-gem cyclobutyl dicarboxylate. Synthesized compounds were evaluated as potential antiviral agents against HIV virus. Some phosphate SATE prodrugs were more active against HIV than parent nucleosides.

摘要

本文描述了一种非常简单的合成新型亲脂性磷酸双(叔丁基-SATE)前药的方法,该前药是由1,1-偕二甲基环丁基二羧酸酯制备的无环环丁基化C-核苷,如异胞嘧啶12和9-脱氮腺嘌呤19。合成的化合物被评估为抗HIV病毒的潜在抗病毒剂。一些磷酸SATE前药对HIV的活性比母体核苷更高。

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