Non-peptide alpha(v)beta(3) antagonists. Part 5: identification of potent RGD mimetics incorporating 2-aryl beta-amino acids as aspartic acid replacements

Bioorg Med Chem Lett. 2002 Dec 2;12(23):3483-6. doi: 10.1016/s0960-894x(02)00743-6.

Abstract

A series of novel, highly potent alpha(v)beta(3) receptor antagonists with favorable pharmacokinetic profiles has been identified. In this series of antagonists, 2-aryl beta-amino acids function as potent aspartic acid replacements.

MeSH terms

  • Amino Acids / chemical synthesis
  • Amino Acids / chemistry*
  • Amino Acids / pharmacokinetics
  • Animals
  • Aspartic Acid / chemistry
  • Biomimetic Materials / chemical synthesis
  • Biomimetic Materials / chemistry
  • Biomimetic Materials / pharmacokinetics
  • Dogs
  • Drug Evaluation, Preclinical
  • Esters / chemical synthesis
  • Esters / chemistry*
  • Esters / pharmacokinetics
  • Humans
  • Inhibitory Concentration 50
  • Oligopeptides / chemistry
  • Oligopeptides / pharmacokinetics
  • Protein Binding
  • Receptors, Vitronectin / antagonists & inhibitors*
  • Receptors, Vitronectin / metabolism
  • Structure-Activity Relationship

Substances

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