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

doi:10.1039/C3OB40624E

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

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* 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.

Organic & Biomolecular Chemistry

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

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

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