Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B

被引：20

作者：

Fraser, Benjamin H. ^{[1
]}

Hamilton, Stephanie ^{[2
]}

Krause-Heuer, Anwen M. ^{[1
]}

Wright, Philip J. ^{[2
]}

Greguric, Ivan ^{[1
]}

Tucker, Simon P. ^{[2
]}

Draffan, Alistair G. ^{[2
]}

Fokin, Valery V. ^{[3
]}

Sharpless, K. Barry ^{[3
]}

机构：

[1] Australian Nucl Sci & Technol Org, Kirrawee Dc, NSW 2232, Australia

[2] Biota Holdings Ltd, Unit 10, Notting Hill, Vic 3168, Australia

[3] Scripps Res Inst, La Jolla, CA 92037 USA

来源：

MEDCHEMCOMM | 2013年 / 4卷 / 02期

关键词：

VIRUS NEURAMINIDASE;

D O I：

10.1039/c2md20300f

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

The copper catalyzed azide alkyne cycloaddition (CuAAC) reaction-the quintessential 'click' reaction-was used to synthesise dimers of the neuraminidase inhibitor zanamivir in high yields. The effect upon anti-viral activity of varying the linker length and the number of triazole units was explored. All dimers were tested for anti-viral activity against influenza A/Sydney/5/97 and B/Harbin/7/94 in a cytopathic effect (CPE) assay.

引用

页码：383 / 386

页数：4

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