Indenone derivatives: a novel template for peroxisome proliferator-activated receptor gamma (PPARgamma) agonists

J Med Chem. 2006 Jul 27;49(15):4781-4. doi: 10.1021/jm060389m.

Abstract

Agonists of peroxisome proliferator-activated receptor gamma (PPAR gamma) are of interest as a treatment for diabetes, which prompted the identification of a new class of non-TZD PPAR gamma agonist. Moreover, compound 14c has displayed the most active agonistic activity with an EC50 value of 50 nM, in addition to exhibiting a new binding mode in the X-ray cocrystal structure.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Crystallography, X-Ray
  • Humans
  • Indenes / chemical synthesis*
  • Indenes / chemistry
  • Indenes / pharmacology
  • Ligands
  • Mice
  • Models, Molecular
  • Molecular Structure
  • NIH 3T3 Cells
  • PPAR gamma / agonists*
  • PPAR gamma / chemistry*

Substances

  • 1-oxo-3-phenyl-6-(3-phenylpropoxy)-1H-indene-2-carboxylic acid ethyl ester
  • Indenes
  • Ligands
  • PPAR gamma