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Issue 2, 2013
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Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B

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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

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Publication details

The article was received on 04 Oct 2012, accepted on 27 Nov 2012 and first published on 29 Nov 2012


Article type: Concise Article
DOI: 10.1039/C2MD20300F
Citation: Med. Chem. Commun., 2013,4, 383-386

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    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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