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

Research output: Contribution to journalArticlepeer-review

27 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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