Synthesis and Anti-HBV Evaluation of 5-Halogenated 2'-Deoxy-2'-β-fluoro-4'-azido Pyrimidine Nucleosides

被引：3

作者：

Guo, Meichao ^{[1
]}

Kang, Jinfeng ^{[1
]}

Hou, Jiao ^{[1
]}

Zhang, Qianqian ^{[1
]}

Yu, Wenquan ^{[1
]}

Chang, Junbiao ^{[1
,2
]}

机构：

[1] Zhengzhou Univ, Coll Chem, Zhengzhou 450001, Peoples R China

[2] Henan Normal Univ, Sch Chem & Chem Engn, Henan Key Lab Organ Funct Mol & Drug Innovat, Xinxiang 453007, Henan, Peoples R China

来源：

CHINESE JOURNAL OF ORGANIC CHEMISTRY | 2020年 / 40卷 / 01期

基金：

中国国家自然科学基金;

关键词：

5-halogenated; pyrimidine nucleoside; synthesis; anti-HBV activity; BIOLOGICAL EVALUATION; ANALOGS; FNC;

D O I：

10.6023/cjoc201907054

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A series of 5-halogenated 2'-deoxy-2'-beta-fluoro-4'-azido pyrimidine nucleosides were synthesized from m-chlorobenzoyl protected 2'-deoxy-2'-beta-fluoro-4'-azido uridine via ammonium cerium nitrate (CAN)-mediated halogenation, activation by triazole, amination, and deprotection. In vitro biological evaluation demonstrated that 5-chloro (6a) and 5-iodo (6c) nucleoside derivatives possess potent anti-HBV (hepatitis B virus) activity with low cytotoxicity.

引用

页码：221 / 225

页数：5

共 12 条

[11] Antiviral activity of FNC, 2′-deoxy-2′-β-fluoro-4′-azidocytidine, against human and duck HBV replication
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[12] Novel nucleoside analogue FNC is effective against both wild-type and lamivudine-resistant HBV clinical isolates
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Zheng, Liyun
Sun, Changyu
Jiang, Jinhua
Yang, Qinghua
Wang, Qingduan
Chang, Junbiao
[J]. ANTIVIRAL THERAPY, 2012, 17 (08) : 1593 - 1599

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