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

MedChemComm Pub Date: 2012-11-29 DOI: 10.1039/C2MD20300F

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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