Design, synthesis, and conformational analysis of a novel series of HIV protease inhibitors

Bioorg Med Chem Lett. 1998 Dec 15;8(24):3631-6. doi: 10.1016/s0960-894x(98)00669-6.

Abstract

A combination of structure-based design and both solution, and solid-phase synthesis were utilized to derive a potent (nM) series of HIV-1 protease inhibitors bearing a structurally novel backbone. Detailed structural analysis of several inhibitors prepared in this series has suggested that rigidification of the P1/P2 region of this class of molecules may result in compounds with improved potency.

MeSH terms

  • Anti-HIV Agents / chemical synthesis*
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology
  • Crystallography, X-Ray
  • Drug Design*
  • HIV Protease Inhibitors / chemical synthesis*
  • HIV Protease Inhibitors / chemistry
  • HIV Protease Inhibitors / pharmacology
  • Models, Molecular
  • Structure-Activity Relationship

Substances

  • Anti-HIV Agents
  • HIV Protease Inhibitors