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Analogs of zanamivir with modified c4-substituents as the inhibitors against the group-1 neuraminidases of influenza viruses

Academic Article
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Overview

authors

  • Wen, W. H.
  • Wang, S. Y.
  • Tsai, K. C.
  • Cheng, Y. S. E.
  • Yang, A. S.
  • Fang, J. M.
  • Wong, Chi-Huey

publication date

  • June 2010

journal

  • Bioorganic & Medicinal Chemistry  Journal

abstract

  • Unlike the group-2 neuraminidase, the group-1 neuraminidase of influenza virus possesses a flexible loop (the 150-loop) and a cavity (the 150-cavity) adjacent to the active site, and renders a conformational change from the 'open' form to the 'closed' form on binding with substrate (sialo-glycoprotein) or inhibitor (e.g., zanamivir). Zanamivir derivative 8a having an extended (piperazinocarbonyl)propyl substituent at the internal N-position of the guanidino group is designed as a possible inhibitor on the basis of computer docking to the open form of N1 subtype neuraminidase. Indeed, compound 8a exhibits strong neuraminidase inhibition and good anti-influenza activity against H1N1 virus with IC(50)=2.15microM and EC(50)=0.77microM, respectively. This study may provide a clue to future design of better group-1 neuraminidase inhibitors.

subject areas

  • Antiviral Agents
  • Enzyme Inhibitors
  • Influenza A Virus, H1N1 Subtype
  • Inhibitory Concentration 50
  • Neuraminidase
  • Orthomyxoviridae
  • Protein Binding
  • Protein Conformation
  • Structure-Activity Relationship
  • Zanamivir
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Research

keywords

  • Influenza
  • Neuraminidase inhibitor
  • Zanamivir derivative
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Identity

International Standard Serial Number (ISSN)

  • 0968-0896

Digital Object Identifier (DOI)

  • 10.1016/j.bmc.2010.04.010

PubMed ID

  • 20452227
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Additional Document Info

start page

  • 4074

end page

  • 4084

volume

  • 18

issue

  • 11

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