The synthesis and evaluation of cyclic ureas as HIV protease inhibitors: modifications of the P1/P1' residues

Bioorg Med Chem Lett. 1998 Apr 7;8(7):823-8. doi: 10.1016/s0960-894x(98)00119-x.

Abstract

Two series of cyclic ureas modified at the P1/P1' residue were prepared and evaluated for HIV protease inhibition and whole cell antiviral activity. Compounds 8b, 10 (3- and 4-pyridylmethyl analogs) and 6b (4-methoxy analog) showed significant improvement in antiviral activity relative to lead compounds DMP323 and DMP 450.

MeSH terms

  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Azepines / pharmacology
  • HIV / drug effects
  • HIV Protease / metabolism
  • HIV Protease Inhibitors / chemical synthesis*
  • HIV Protease Inhibitors / chemistry
  • HIV Protease Inhibitors / pharmacology
  • Indicators and Reagents
  • Kinetics
  • Molecular Structure
  • Structure-Activity Relationship
  • Urea / analogs & derivatives*
  • Urea / chemical synthesis*
  • Urea / chemistry
  • Urea / pharmacology

Substances

  • Antiviral Agents
  • Azepines
  • HIV Protease Inhibitors
  • Indicators and Reagents
  • Urea
  • HIV Protease
  • DMP 323
  • DMP 450