Imidazopyridines as VLA-4 integrin antagonists

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4146-9. doi: 10.1016/j.bmcl.2008.05.075. Epub 2008 May 23.

Abstract

We describe a novel series of imidazopyridine substituted phenylalanines which are potent VLA-4 antagonists. A wide variety of substituents are tolerated as replacements for the pendant 3-pyridyl ring. A clear structure-activity relationship was identified around the substitution of the 3-amino-cyclobut-2-enone portion of the molecule.

MeSH terms

  • Animals
  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Humans
  • Inhibitory Concentration 50
  • Integrin alpha4beta1 / antagonists & inhibitors*
  • Integrin alpha4beta1 / blood
  • Mice
  • Models, Chemical
  • Molecular Conformation
  • Phenylalanine / chemistry*
  • Protein Binding
  • Pyridines / chemistry*
  • Rats
  • Structure-Activity Relationship

Substances

  • Integrin alpha4beta1
  • Pyridines
  • Phenylalanine