Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120)

Bioorg Med Chem Lett. 2014 Jul 15;24(14):3100-3. doi: 10.1016/j.bmcl.2014.05.012. Epub 2014 May 16.

Abstract

The exploration of a diarylsulfonamide series of free fatty acid receptor 4 (FFA4/GPR120) agonists is described. This work led to the identification of selective FFA4 agonist 8 (GSK137647A) and selective FFA4 antagonist 39. The in vitro profile of compounds 8 and 39 is presented herein.

Keywords: FFA4; Free fatty acid receptor 4; Free fatty acid receptor 4 agonist; Free fatty acid receptor 4 antagonist; GPR120.

MeSH terms

  • Animals
  • Cell Line
  • Dose-Response Relationship, Drug
  • HEK293 Cells
  • Humans
  • Insulin / agonists
  • Mice
  • Molecular Structure
  • Receptors, G-Protein-Coupled / agonists*
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*

Substances

  • FFAR4 protein, human
  • Insulin
  • Receptors, G-Protein-Coupled
  • Sulfonamides