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某些4'-硫代-2'-脱氧核苷类似物的合成与抗病毒活性

The synthesis and antiviral activity of some 4'-thio-2'-deoxy nucleoside analogues.

作者信息

Dyson M R, Coe P L, Walker R T

机构信息

School of Chemistry, University of Birmingham, England.

出版信息

J Med Chem. 1991 Sep;34(9):2782-6. doi: 10.1021/jm00113a016.

Abstract

Starting from benzyl 3,5-di-O-benzyl-2-deoxy-1,4-dithio-D-erythro- pentofuranoside (4), the following 2'-deoxy nucleoside analogues have been synthesized: 4'-thiothymidine (8), 3'-azido-4'-thio- deoxythymidine (10), and (E)-5-(2-bromovinyl)-4'-thio-2'-deoxyuridine (22). The first compound is toxic, the second is not toxic nor has detectable biological activity, and the third is not toxic and has significant activity against some herpesviruses.

摘要

从苄基3,5 - 二 - O - 苄基 - 2 - 脱氧 - 1,4 - 二硫代 - D - 赤藓糖基呋喃糖苷(4)开始,已合成了以下2'-脱氧核苷类似物:4'-硫代胸苷(8)、3'-叠氮基 - 4'-硫代脱氧胸苷(10)和(E)-5 - (2 - 溴乙烯基)-4'-硫代 - 2'-脱氧尿苷(22)。第一种化合物有毒,第二种无毒且没有可检测到的生物活性,第三种无毒且对某些疱疹病毒具有显著活性。

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