N-acyl phenylalanine analogues as potent small molecule VLA-4 antagonists

Bioorg Med Chem Lett. 2000 Apr 17;10(8):725-7. doi: 10.1016/s0960-894x(00)00088-3.

Abstract

We have identified a series of low molecular weight (Mr < 500) N-acylphenylalanines that are effective inhibitors of the VCAM-VLA-4 interaction. Investigation of the SAR of the N-acyl moiety led to the identification of N-benzylpyroglutamyl derivatives as being particularly potent.

MeSH terms

  • Acylation
  • Integrin alpha4beta1
  • Integrins / antagonists & inhibitors*
  • Phenylalanine / analogs & derivatives*
  • Phenylalanine / pharmacology*
  • Receptors, Lymphocyte Homing / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Integrin alpha4beta1
  • Integrins
  • Receptors, Lymphocyte Homing
  • Phenylalanine