Non-peptide alpha(v)beta(3) antagonists. Part 3: identification of potent RGD mimetics incorporating novel beta-amino acids as aspartic acid replacements

Bioorg Med Chem Lett. 2002 Jan 7;12(1):31-4. doi: 10.1016/s0960-894x(01)00666-7.

Abstract

Potent non-peptidic alpha(v)beta(3) antagonists have been prepared incorporating various beta-amino acids as aspartic acid mimetics. Modification of the beta-alanine 3-substituents alters the potency and physicochemical properties of these receptor antagonists and in some cases provides orally bioavailable alpha(v)beta(3) inhibitors.

MeSH terms

  • Amino Acids / chemistry
  • Animals
  • Aspartic Acid
  • Binding, Competitive
  • Dogs
  • Drug Evaluation, Preclinical
  • Humans
  • Inhibitory Concentration 50
  • Molecular Mimicry
  • Oligopeptides / administration & dosage
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacokinetics*
  • Osteoporosis / prevention & control
  • Protein Binding
  • Receptors, Vitronectin / antagonists & inhibitors*
  • Receptors, Vitronectin / metabolism
  • Structure-Activity Relationship

Substances

  • Amino Acids
  • Oligopeptides
  • Receptors, Vitronectin
  • Aspartic Acid
  • arginyl-glycyl-aspartic acid