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
收藏
页码：383 / 386
页数：4
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