Squaric acid derivatives as VLA-4 integrin antagonists

Bioorg Med Chem Lett. 2002 Apr 8;12(7):1051-4. doi: 10.1016/s0960-894x(02)00075-6.

Abstract

SAR studies aimed at improving the rate of clearance by the incorporation of a 3,4-diamino-3-cyclobutene-1,2-dione group as an amino acid isostere in a series of VLA-4 integrin antagonists are described.

MeSH terms

  • Amines / chemistry
  • Animals
  • Anti-Allergic Agents / antagonists & inhibitors*
  • Cyclobutanes / chemical synthesis*
  • Cyclobutanes / pharmacology*
  • Integrin alpha4beta1
  • Integrin beta1
  • Integrins / antagonists & inhibitors*
  • Metabolic Clearance Rate
  • Rats
  • Receptors, Lymphocyte Homing / antagonists & inhibitors*
  • Receptors, Very Late Antigen
  • Structure-Activity Relationship

Substances

  • Amines
  • Anti-Allergic Agents
  • Cyclobutanes
  • Integrin alpha4beta1
  • Integrin beta1
  • Integrins
  • Receptors, Lymphocyte Homing
  • Receptors, Very Late Antigen
  • squaric acid