Lysine sulfonamides as novel HIV-protease inhibitors: Nepsilon-acyl aromatic alpha-amino acids

Bioorg Med Chem Lett. 2006 Jul 1;16(13):3459-62. doi: 10.1016/j.bmcl.2006.04.011. Epub 2006 Apr 27.

Abstract

A series of lysine sulfonamide analogues bearing Nepsilon-acyl aromatic amino acids were synthesized using an efficient synthetic route. Evaluation of these novel protease inhibitors revealed compounds with high potency against wild-type and multiple-protease inhibitor-resistant HIV viruses.

MeSH terms

  • Acylation
  • Amino Acids / chemistry*
  • Anti-HIV Agents / chemical synthesis
  • Anti-HIV Agents / chemistry
  • Anti-HIV Agents / pharmacology*
  • Cell Line
  • Drug Design
  • Drug Evaluation, Preclinical
  • HIV / drug effects
  • HIV Protease Inhibitors / chemical synthesis
  • HIV Protease Inhibitors / chemistry
  • HIV Protease Inhibitors / pharmacology*
  • Humans
  • In Vitro Techniques
  • Lysine / analogs & derivatives
  • Lysine / chemistry*
  • Microbial Sensitivity Tests
  • Molecular Structure
  • Stereoisomerism
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*

Substances

  • Amino Acids
  • Anti-HIV Agents
  • HIV Protease Inhibitors
  • Sulfonamides
  • Lysine