Potent HIV-1 protease inhibitors with antiviral activities in vitro

Biochem Biophys Res Commun. 1991 Mar 29;175(3):914-9. doi: 10.1016/0006-291x(91)91652-s.

Abstract

A series of novel difluoroketones with low molecular weight (less than 600 m.u.) and which are potent inhibitors of the HIV-1 protease (IC50 = 1.0 to 21 nM) were synthesized. These compounds also exhibited antiviral activity by inhibition of the cytopathic effect of HIV-1(3)B in MT-4 cells in vitro.

Publication types

  • Comparative Study

MeSH terms

  • Antiviral Agents / chemical synthesis
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology*
  • Cell Line
  • HIV Protease Inhibitors*
  • HIV-1 / drug effects
  • HIV-1 / enzymology*
  • Humans
  • Ketones / chemical synthesis
  • Ketones / chemistry
  • Ketones / pharmacology
  • Molecular Structure
  • Protease Inhibitors / chemical synthesis
  • Protease Inhibitors / pharmacology*
  • Recombinant Proteins / antagonists & inhibitors
  • Structure-Activity Relationship

Substances

  • Antiviral Agents
  • HIV Protease Inhibitors
  • Ketones
  • Protease Inhibitors
  • Recombinant Proteins