Syntheses of triazole-modified zanamivir analogues via click chemistry and anti-AIV activities

  • Bioorg Med Chem Lett. 2006 Oct 1;16(19):5009-13. doi: 10.1016/j.bmcl.2006.07.047.
Jian Li  1 ,  Mingyue Zheng ,  Wei Tang ,  Pei-Lan He ,  Weiliang Zhu ,  Tianxian Li ,  Jian-Ping Zuo ,  Hong Liu ,  Hualiang Jiang
Affiliations
  • 1. Drug Discovery and Design Centre, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, Shanghai 201203, China.
PMID: 16876409 DOI: 10.1016/j.bmcl.2006.07.047
Abstract

Sixteen novel 4-triazole-modified zanamivir (1) analogues were synthesized using the click reactions, and their inhibitory activities against avian Influenza Virus (AIV, H5N1) were determined. Compound 3b exerts promising inhibitory activity with EC(50) of 6.4 microM, which is very close to that of zanamivir (EC(50) = 2.8 microM). Molecular modeling provided the information about the binding model between inhibitors and neuraminidase, which are in good agreement with inhibitory activities.