N-aryl 2,6-dimethoxybiphenylalanine analogues as VLA-4 antagonists

Bioorg Med Chem Lett. 2002 Mar 11;12(5):729-31. doi: 10.1016/s0960-894x(02)00009-4.

Abstract

A series of N-arylated phenylalanine derivatives has been synthesized and has been shown to be potent inhibitors of the integrin VLA-4. N-phenyl and N-heteroaryl derivatives with hydrogen bond acceptors in the meta position demonstrated low nanomolar activity against VLA-4.

MeSH terms

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

Substances

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