A series of C-terminal amino alcohol dipeptide A beta inhibitors

Bioorg Med Chem Lett. 2002 Nov 4;12(21):3051-3. doi: 10.1016/s0960-894x(02)00684-4.

Abstract

Potent, small molecule A beta inhibitors have been prepared that incorporate an alanine core bracketed by an N-terminal arylacetyl group and various C-terminal amino alcohols. The compounds exhibit stereospecific inhibition as demonstrated in an in vitro assay.

MeSH terms

  • Amino Alcohols / chemical synthesis*
  • Amino Alcohols / pharmacology*
  • Amyloid Precursor Protein Secretases
  • Amyloid beta-Peptides / antagonists & inhibitors*
  • Amyloid beta-Peptides / genetics
  • Aspartic Acid Endopeptidases
  • Cell Line
  • Cell Survival / drug effects
  • Dipeptides / chemical synthesis*
  • Dipeptides / pharmacology*
  • Endopeptidases / metabolism
  • Humans
  • Mutation
  • Structure-Activity Relationship
  • Transfection

Substances

  • Amino Alcohols
  • Amyloid beta-Peptides
  • Dipeptides
  • Amyloid Precursor Protein Secretases
  • Endopeptidases
  • Aspartic Acid Endopeptidases
  • BACE1 protein, human