2,3-Benzodiazepin-1,4-diones as peptidomimetic inhibitors of gamma-secretase

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3535-8. doi: 10.1016/j.bmcl.2004.04.056.

Abstract

2,3-Benzodiazepin-1,4-diones were designed as peptidomimetics at the carboxy terminus of hydroxyamides. Inhibition of brain Abeta production was improved by one of the compounds containing constrained modification.

Publication types

  • Comparative Study

MeSH terms

  • Alzheimer Disease / enzymology
  • Amides / chemistry
  • Amyloid Precursor Protein Secretases
  • Animals
  • Aspartic Acid Endopeptidases
  • Benzodiazepines / chemical synthesis
  • Benzodiazepines / pharmacology
  • Brain / drug effects*
  • Brain / metabolism
  • Cell Line
  • Drug Design
  • Endopeptidases / metabolism*
  • Inhibitory Concentration 50
  • Ketones / chemical synthesis
  • Ketones / pharmacology
  • Mice
  • Molecular Conformation
  • Molecular Mimicry
  • Protease Inhibitors / chemical synthesis
  • Protease Inhibitors / pharmacology*
  • Protein Binding

Substances

  • Amides
  • Ketones
  • Protease Inhibitors
  • Benzodiazepines
  • Amyloid Precursor Protein Secretases
  • Endopeptidases
  • Aspartic Acid Endopeptidases
  • Bace1 protein, mouse