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新型亚甲基无环核苷和膦酸核苷的合成及抗病毒评价

Synthesis and antiviral evaluation of novel exomethylene acyclic nucleosides and phosphonic acid nucleosides.

作者信息

Kim Aihong, Hong Joon Hee

机构信息

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

出版信息

Arch Pharm (Weinheim). 2005 Nov;338(11):528-33. doi: 10.1002/ardp.200500187.

DOI:10.1002/ardp.200500187
PMID:16281311
Abstract

This paper describes a very simple synthesis route of novel acyclic nucleosides and phosphonic acid nucleosides. The condensation of the mesylates 6 and 17 with the natural nucleosidic bases (A, C, U, T) under nucleophilic substitution (K(2)CO(3), 18-Crown-6, DMF) and deprotection afforded the target nucleosides (11, 12, 13, 14) and phosphonic acid nucleosides (22, 23, 24, 25). In addition, these compounds were evaluated for their antiviral properties against various viruses. Uracil derivative 24 shows significant anti-HCMV activity (EC(50) = 10.24 microM).

摘要

本文描述了一种新型无环核苷和膦酸核苷的非常简单的合成路线。甲磺酸酯6和17与天然核苷碱基（A、C、U、T）在亲核取代反应（K₂CO₃、18-冠醚-6、N,N-二甲基甲酰胺）条件下缩合并脱保护，得到目标核苷（11、12、13、14）和膦酸核苷（22、23、24、25）。此外，对这些化合物针对多种病毒的抗病毒特性进行了评估。尿嘧啶衍生物24显示出显著的抗人巨细胞病毒活性（半数有效浓度=10.24微摩尔/升）。

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