Issue 2, 2013

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

Abstract

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.

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

Supplementary files

Article information

Article type
Concise Article
Submitted
04 Oct 2012
Accepted
27 Nov 2012
First published
29 Nov 2012

Med. Chem. Commun., 2013,4, 383-386

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

B. H. Fraser, S. Hamilton, A. M. Krause-Heuer, P. J. Wright, I. Greguric, S. P. Tucker, A. G. Draffan, V. V. Fokin and K. B. Sharpless, Med. Chem. Commun., 2013, 4, 383 DOI: 10.1039/C2MD20300F

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