Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities

Chien Hung Lin, Tsung Che Chang, Anindya Das, Ming Yu Fang, Hui Chen Hung, Kai Cheng Hsu, Jinn Moon Yang, Mark Von Itzstein, Kwok Kong T Mong, Tsu An Hsu, Chun Cheng Lin

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26 Citations (Scopus)

Abstract

A series of acylguanidine-modified zanamivir analogs were synthesized and their inhibitory activities against the NAs of avian influenza viruses (H1N1 and H3N2) were evaluated. In particular, zanamivir derivative 3j, with a hydrophobic naphthalene substituent, exhibits the best inhibitory activity against group-1 NA with an IC50 of 20 nM.

Original languageEnglish
Pages (from-to)3943-3948
Number of pages6
JournalOrganic and Biomolecular Chemistry
Volume11
Issue number24
DOIs
Publication statusPublished - Jun 28 2013
Externally publishedYes

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Biochemistry

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  • Cite this

    Lin, C. H., Chang, T. C., Das, A., Fang, M. Y., Hung, H. C., Hsu, K. C., Yang, J. M., Von Itzstein, M., Mong, K. K. T., Hsu, T. A., & Lin, C. C. (2013). Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities. Organic and Biomolecular Chemistry, 11(24), 3943-3948. https://doi.org/10.1039/c3ob40624e