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[类似于阿昔洛韦的化合物。VIII. 核酸碱基的 (R/S)-5-羟基-4-羟甲基-3-氧杂戊-2-基衍生物的合成及抗病毒活性]

[Compounds, similar to acyclovir. VIII. Synthesis and antiviral activity of (R/S)-5-hydroxy-4-hydroxymethyl-3-oxapent-2-yl derivatives of nucleic bases].

作者信息

Smirnov I P, Tsilevich T L, Kochetkova S V, Vladyko G V, Korobchenko L V, Boreko E I, Gottikh B P, Florent'ev V L

出版信息

Bioorg Khim. 1993 Jan;19(1):95-102.

PMID:8387307
Abstract

The (R/S)-5-hydroxy-4-hydroxymethyl-3-oxapent-2-yl derivatives of the uracil, thymidine, cytosine, adenine, guanine and 1,2,4-triazol-3-carboxamide were synthesized using 1,3-diacetoxy-2-(1-acetoxy)propane and 1,3-dichloro-2-(1-chlorethoxy)propane as alkylating agents. The guanine derivatives exhibited activity against HSV-1 (chemotherapeutic index 32).

摘要

使用1,3 - 二乙酰氧基 - 2 -（1 - 乙酰氧基）丙烷和1,3 - 二氯 - 2 -（1 - 氯乙氧基）丙烷作为烷基化剂，合成了尿嘧啶、胸苷、胞嘧啶、腺嘌呤、鸟嘌呤和1,2,4 - 三唑 - 3 - 甲酰胺的（R/S）-5 - 羟基 - 4 - 羟甲基 - 3 - 氧杂戊 - 2 - 基衍生物。鸟嘌呤衍生物对单纯疱疹病毒1型表现出活性（化疗指数为32）。

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