Nonsymmetrically substituted cyclic urea HIV protease inhibitors

J Med Chem. 1997 Dec 5;40(25):4079-88. doi: 10.1021/jm970288b.

Abstract

A series of nonsymmetrically substituted cyclic ureacarboxamides was synthesized and evaluated for antiviral activity as a function of the inhibition of HIV-protease. Selected protease inhibitors were also evaluated for oral bioavailability. The synthesis, pharmacology, quantitative structure-activity relationship (QSAR), and pharmacokinetics for the series will be discussed.

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / pharmacokinetics
  • Anti-HIV Agents / pharmacology
  • HIV Protease Inhibitors / chemical synthesis*
  • HIV Protease Inhibitors / pharmacokinetics
  • HIV Protease Inhibitors / pharmacology
  • RNA, Viral / analysis
  • Structure-Activity Relationship
  • Urea / chemical synthesis*
  • Urea / pharmacokinetics
  • Urea / pharmacology

Substances

  • Anti-HIV Agents
  • HIV Protease Inhibitors
  • RNA, Viral
  • Urea