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 journalArticle

21 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

Fingerprint

Zanamivir
Neuraminidase
Bioactivity
inhibitors
Derivatives
influenza
Influenza in Birds
evaluation
viruses
synthesis
Orthomyxoviridae
Viruses
naphthalene
Inhibitory Concentration 50
analogs

ASJC Scopus subject areas

  • Physical and Theoretical Chemistry
  • Organic Chemistry
  • Biochemistry

Cite this

Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities. / Lin, Chien Hung; Chang, Tsung Che; Das, Anindya; Fang, Ming Yu; Hung, Hui Chen; Hsu, Kai Cheng; Yang, Jinn Moon; Von Itzstein, Mark; Mong, Kwok Kong T; Hsu, Tsu An; Lin, Chun Cheng.

In: Organic and Biomolecular Chemistry, Vol. 11, No. 24, 28.06.2013, p. 3943-3948.

Research output: Contribution to journalArticle

Lin, CH, Chang, TC, Das, A, Fang, MY, Hung, HC, Hsu, KC, Yang, JM, Von Itzstein, M, Mong, KKT, Hsu, TA & Lin, CC 2013, 'Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities', Organic and Biomolecular Chemistry, vol. 11, no. 24, pp. 3943-3948. https://doi.org/10.1039/c3ob40624e
Lin, Chien Hung ; Chang, Tsung Che ; Das, Anindya ; Fang, Ming Yu ; Hung, Hui Chen ; Hsu, Kai Cheng ; Yang, Jinn Moon ; Von Itzstein, Mark ; Mong, Kwok Kong T ; Hsu, Tsu An ; Lin, Chun Cheng. / Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities. In: Organic and Biomolecular Chemistry. 2013 ; Vol. 11, No. 24. pp. 3943-3948.
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