N-aryl-prolyl-dipeptides as potent antagonists of VLA-4

Bioorg Med Chem Lett. 2002 Aug 19;12(16):2205-8. doi: 10.1016/s0960-894x(02)00356-6.

Abstract

The design, synthesis, and biological evaluation of N-arylprolyl-dipeptide derivatives as small molecule VLA-4 antagonists is described. Potency against VLA-4 and alpha(4)beta(7) and rat pharmacokinetic evaluation revealed some advantages over the related N-(arylsulfonyl)-prolyl-dipeptide analogues.

MeSH terms

  • Animals
  • Dipeptides / blood
  • Dipeptides / chemical synthesis*
  • Dipeptides / pharmacokinetics
  • Dipeptides / pharmacology*
  • Half-Life
  • Integrin alpha4beta1 / antagonists & inhibitors*
  • Metabolic Clearance Rate
  • Molecular Structure
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship

Substances

  • Dipeptides
  • Integrin alpha4beta1