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

…, AM Krause-Heuer, PJ Wright, I Greguric, SP Tucker…

Index: 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 MedChemComm, 2013 , vol. 4, # 2 p. 383 - 386

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Citation Number: 7

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.