Potent and Selective Biphenyl Azole Inhibitors of Adipocyte Fatty Acid Binding Protein (aFABP)

Bioorg Med Chem Lett. 2007 Jun 15;17(12):3511-5. doi: 10.1016/j.bmcl.2006.12.044. Epub 2006 Dec 21.

Abstract

Herein we report the first disclosure of biphenyl azoles that are nanomolar binders of adipocyte fatty acid binding protein (aFABP or aP2) with up to thousand-fold selectivity against muscle fatty acid binding protein and epidermal fatty acid binding protein. In addition a new radio-ligand to determine binding against the three fatty acid binding proteins was also synthesized.

MeSH terms

  • Adipocytes / drug effects*
  • Adipocytes / metabolism
  • Animals
  • Azoles / antagonists & inhibitors*
  • Binding Sites
  • Biphenyl Compounds / antagonists & inhibitors*
  • Disease Models, Animal
  • Epidermis / metabolism
  • Fatty Acid-Binding Proteins / antagonists & inhibitors*
  • Hypoglycemic Agents / chemical synthesis
  • Hypoglycemic Agents / pharmacology*
  • Hypolipidemic Agents / chemical synthesis
  • Hypolipidemic Agents / pharmacology*
  • Mice
  • Models, Chemical
  • Radioligand Assay

Substances

  • Azoles
  • Biphenyl Compounds
  • Fatty Acid-Binding Proteins
  • Hypoglycemic Agents
  • Hypolipidemic Agents
  • diphenyl