Issue 24, 2013
From the journal:

Organic & Biomolecular Chemistry

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

Chien-Hung Lin,a   Tsung-Che Chang,a   Anindya Das,a   Ming-Yu Fang,b   Hui-Chen Hung,b   Kai-Cheng Hsu,c   Jinn-Moon Yang,c   Mark von Itzstein,d   Kwok Kong T. Mong,c   Tsu-An Hsu*b  and  Chun-Cheng Lin*a  

* Corresponding authors

a Department of Chemistry, National Tsing Hua University, 101, Section 2, Kuang-Fu Road, Hsinchu 30013, Taiwan

b Division of Biotechnology and Pharmaceutical Research, National Health Research Institutes, 35, Keyan Road, Zhunan 35053, Taiwan

c Department of Biological Science and Technology and Applied Chemistry Department, National Chiao Tung University, University Road, Hsinchu 30010, Taiwan

d Institute for Glycomics, Griffith University (Gold Coast Campus), Southport, Queensland 4222, Australia
E-mail: cclin66@mx.nthu.edu.tw
Fax: +886 3-571-1082

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.

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

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Article information

DOI
https://doi.org/10.1039/C3OB40624E
Article type
Communication
Submitted
28 Mar 2013
Accepted
09 May 2013
First published
10 May 2013

Org. Biomol. Chem., 2013,11, 3943-3948

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

C. Lin, T. Chang, A. Das, M. Fang, H. Hung, K. Hsu, J. Yang, M. von Itzstein, K. K. T. Mong, T. Hsu and C. Lin, Org. Biomol. Chem., 2013, 11, 3943 DOI: 10.1039/C3OB40624E

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