Identification of novel epoxide inhibitors of hepatitis C virus replication using a high-throughput screen

Antimicrob Agents Chemother. 2007 Oct;51(10):3756-9. doi: 10.1128/AAC.00233-07. Epub 2007 Aug 6.

Abstract

Using our high-throughput hepatitis C replicon assay to screen a library of over 8,000 novel diversity-oriented synthesis (DOS) compounds, we identified several novel compounds that regulate hepatitis C virus (HCV) replication, including two libraries of epoxides that inhibit HCV replication (best 50% effective concentration, < 0.5 microM). We then synthesized an analog of these compounds with optimized activity.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / pharmacology*
  • Computer Simulation
  • Cytopathogenic Effect, Viral / drug effects
  • Drug Design
  • Drug Evaluation, Preclinical
  • Epoxy Compounds / chemical synthesis*
  • Epoxy Compounds / pharmacology*
  • Hepacivirus / drug effects*
  • Maleimides / pharmacology
  • Replicon / drug effects
  • Reproducibility of Results
  • Structure-Activity Relationship
  • Virus Replication / drug effects*

Substances

  • Antiviral Agents
  • Epoxy Compounds
  • Maleimides
  • maleimide