1,3,5-Trisubstituted aryls as highly selective PPARdelta agonists

Bioorg Med Chem Lett. 2006 Jun 1;16(11):2969-73. doi: 10.1016/j.bmcl.2006.02.079. Epub 2006 Mar 20.

Abstract

A series of highly potent and selective PPARdelta agonists is described using the known non-selective ligand GW2433 as a structural template. Compound 1 is bioavailable, potent (10 nM), and shows no cross-activity with other PPAR subtypes up to 10 microM, making it a useful tool in studying the biological effects of selective PPARdelta activation.

MeSH terms

  • Butyrates / chemistry*
  • Butyrates / metabolism*
  • Ligands
  • Models, Molecular
  • Molecular Structure
  • PPAR delta / agonists*
  • PPAR delta / chemistry
  • PPAR delta / metabolism*
  • Phenylurea Compounds / chemistry*
  • Phenylurea Compounds / metabolism*
  • Structure-Activity Relationship

Substances

  • Butyrates
  • GW 2433
  • Ligands
  • PPAR delta
  • Phenylurea Compounds