A small-molecule inhibitor of Nipah virus envelope protein-mediated membrane fusion

J Med Chem. 2009 Jul 23;52(14):4257-65. doi: 10.1021/jm900411s.

Abstract

Nipah virus (NiV), a highly pathogenic paramyxovirus, causes respiratory disease in pigs and severe febrile encephalitis in humans with high mortality rates. On the basis of the structural similarity of viral fusion (F) proteins within the family Paramyxoviridae, we designed and tested 18 quinolone derivatives in a NiV and measles virus (MV) envelope protein-based fusion assay beside evaluation of cytotoxicity. We found five compounds successfully inhibiting NiV envelope protein-induced cell fusion. The most active molecules (19 and 20), which also inhibit the syncytium formation induced by infectious NiV and show a low cytotoxicity in Vero cells, represent a promising lead quinolone-type compound structure. Molecular modeling indicated that compound 19 fits well into a particular protein cavity present on the NiV F protein that is important for the fusion process.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Cell Line
  • Chlorocebus aethiops
  • Computer Simulation
  • Dogs
  • Dose-Response Relationship, Drug
  • Humans
  • Measles virus / drug effects
  • Measles virus / metabolism
  • Measles virus / physiology
  • Models, Molecular
  • Molecular Conformation
  • Nipah Virus / drug effects
  • Nipah Virus / metabolism
  • Nipah Virus / physiology*
  • Quinolones / chemistry
  • Quinolones / pharmacology
  • Viral Envelope Proteins / chemistry
  • Viral Envelope Proteins / metabolism*
  • Virus Internalization / drug effects*

Substances

  • Quinolones
  • Viral Envelope Proteins