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 Mong, Tsu An Hsu*, Chun Cheng Lin

*Corresponding author for this work

Research output: Contribution to journalArticle

26 Scopus citations

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
StatePublished - 28 Jun 2013

Fingerprint Dive into the research topics of 'Synthesis of acylguanidine zanamivir derivatives as neuraminidase inhibitors and the evaluation of their bio-activities'. Together they form a unique fingerprint.

Cite this