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芹菜糖基核苷4'和5'-修饰类似物作为强效抗丙型肝炎病毒药物的合成及体外活性

Synthesis and in vitro activity of 4' and 5'-modified analogues of apiosyl nucleosides as potent anti-HCV agents.

作者信息

Li Hua, Lee Wonjae, Hong Joon Hee

机构信息

BK21-Project Team, College of Pharmacy, Chosun University, Kwangju, Republic of Korea.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2009 Nov;28(11):1104-16. doi: 10.1080/15257770903396725.

DOI:10.1080/15257770903396725
PMID:20183577
Abstract

Novel doubly branched apio dideoxynucleosides were synthesized starting from 1,3-dihydroxyacetone using an ozonolysis and Grignard addition as key steps, and evaluated for anti-hepatitis C virus (HCV) activity. The adenine derivative 24 showed significant anti-HCV activity, indicating that the branches at the 4',5'-position of the apiosyl ring led to favorable interaction with HCV polymerase.

摘要

以1,3 - 二羟基丙酮为起始原料，通过臭氧分解和格氏加成作为关键步骤合成了新型双分支阿皮二脱氧核苷，并对其抗丙型肝炎病毒（HCV）活性进行了评估。腺嘌呤衍生物24表现出显著的抗HCV活性，表明阿皮糖环4'，5'-位的分支与HCV聚合酶产生了有利的相互作用。

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