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

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. © Royal Society of Chemistry

Keywords

Synthesis, Triazoles, Dimers, Influenza, Enzyme inhibitors, Viruses, Lungs

Citation

Fraser, B. H., Hamilton, S., Krause-Heuer, A. M., Wright, P. J., Greguric, I., Tucker, S. P., Draffan, A. G., Fokin, V. V., & Sharpless, K. B. (2013). Synthesis of 1, 4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B. MedChemComm, 4(2), 383-386. doi.10.1039/C2MD20300F