Inhibitors of Hepatitis C Virus NS3.4A Protease 1. Non-charged Tetrapeptide Variants

Bioorg Med Chem Lett. 2003 Nov 17;13(22):4059-63. doi: 10.1016/j.bmcl.2003.08.050.

Abstract

Tetrapeptide-based peptidomimetic compounds have been shown to effectively inhibit the hepatitis C virus NS3.4A protease without the need of a charged functionality. An aldehyde is used as a prototype reversible electrophilic warhead. The SAR of the P1 and P2 inhibitor positions is discussed.

MeSH terms

  • Hepacivirus / drug effects
  • Hepacivirus / enzymology*
  • Kinetics
  • Models, Molecular
  • Oligopeptides / chemical synthesis*
  • Oligopeptides / pharmacology*
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / pharmacology
  • Protein Conformation
  • Structure-Activity Relationship
  • X-Ray Diffraction

Substances

  • Oligopeptides
  • Protease Inhibitors