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

Research output: Contribution to journalArticle

10 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

Fingerprint

Zanamivir
Triazoles
Alkynes
Azides
Cycloaddition Reaction
Neuraminidase
Dimers
Human Influenza
Copper
Cycloaddition
Assays

ASJC Scopus subject areas

  • Biochemistry
  • Pharmaceutical Science

Cite this

Fraser, B. H., Hamilton, S., Krause-Heuer, A. M., Wright, P. J., Greguric, I., Tucker, S. P., ... 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

Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B. / Fraser, Benjamin H.; Hamilton, Stephanie; Krause-Heuer, Anwen M.; Wright, Philip J.; Greguric, Ivan; Tucker, Simon P.; Draffan, Alistair G.; Fokin, Valery V.; Sharpless, K. Barry.

In: MedChemComm, Vol. 4, No. 2, 2013, p. 383-386.

Research output: Contribution to journalArticle

Fraser, BH, Hamilton, S, Krause-Heuer, AM, Wright, PJ, Greguric, I, Tucker, SP, Draffan, AG, Fokin, VV & Sharpless, KB 2013, 'Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B', MedChemComm, vol. 4, no. 2, pp. 383-386. https://doi.org/10.1039/c2md20300f
Fraser BH, Hamilton S, Krause-Heuer AM, Wright PJ, Greguric I, Tucker SP et al. Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B. MedChemComm. 2013;4(2):383-386. https://doi.org/10.1039/c2md20300f
Fraser, Benjamin H. ; Hamilton, Stephanie ; Krause-Heuer, Anwen M. ; Wright, Philip J. ; Greguric, Ivan ; Tucker, Simon P. ; Draffan, Alistair G. ; Fokin, Valery V. ; Sharpless, K. Barry. / Synthesis of 1,4-triazole linked zanamivir dimers as highly potent inhibitors of influenza A and B. In: MedChemComm. 2013 ; Vol. 4, No. 2. pp. 383-386.
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