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

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.
AuthorsJian Li, Mingyue Zheng, Wei Tang, Pei-Lan He, Weiliang Zhu, Tianxian Li, Jian-Ping Zuo, Hong Liu, Hualiang Jiang
JournalBioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 16 Issue 19 Pg. 5009-13 (Oct 01 2006) ISSN: 0960-894X [Print] England
PMID16876409 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • Antiviral Agents
  • Enzyme Inhibitors
  • Guanidines
  • Pyrans
  • Sialic Acids
  • Triazoles
  • Neuraminidase
  • Zanamivir
Topics
  • Antiviral Agents (chemical synthesis, pharmacology)
  • Enzyme Inhibitors (chemistry, metabolism)
  • Guanidines (chemical synthesis, chemistry, pharmacology)
  • Humans
  • Influenza A Virus, H5N1 Subtype (drug effects)
  • Influenza, Human (prevention & control)
  • Models, Molecular
  • Neuraminidase (antagonists & inhibitors, metabolism)
  • Pyrans (chemical synthesis, chemistry, pharmacology)
  • Sialic Acids (chemical synthesis, chemistry, pharmacology)
  • Structure-Activity Relationship
  • Triazoles
  • Zanamivir

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