Synthesis of novel cyclic urea based HIV-1 protease inhibitors

Drug Des Discov. 1995 Nov;13(2):83-7.

Abstract

A series of novel HIV-1 protease inhibitors was prepared in a short stereospecific manner. These compounds have only one P1 substituent interacting with the S1/S1' binding site of HIV-1 protease and only one hydroxyl group interacting with the catalytic aspartic acid domain, X-ray crystallography confirmed the desired R, R configuration of the final products.

MeSH terms

  • Crystallography, X-Ray
  • Cyclization
  • HIV Protease Inhibitors / chemical synthesis*
  • HIV Protease Inhibitors / pharmacology
  • HIV-1 / drug effects*
  • HIV-1 / enzymology*
  • Isomerism
  • Molecular Conformation
  • Urea / analogs & derivatives
  • Urea / chemical synthesis*

Substances

  • HIV Protease Inhibitors
  • Urea