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

Benjamin H. Fraser, Stephanie Hamilton, Anwen M. Krause-Heuer, Philip J. Wright, Ivan Greguric, Simon P. Tucker, Alistair G. Draffan, Valery V. Fokin, K. Barry Sharpless

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13 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)383-386
Number of pages4
JournalMedChemComm
Volume4
Issue number2
DOIs
Publication statusPublished - 2013
Externally publishedYes

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

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    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. https://doi.org/10.1039/c2md20300f