Truxillic acid derivatives act as peroxisome proliferator-activated receptor gamma activators

Bioorg Med Chem Lett. 2010 May 1;20(9):2920-3. doi: 10.1016/j.bmcl.2010.03.026. Epub 2010 Mar 7.

Abstract

In previous studies, we identified a truxillic acid derivative as selective activator of the peroxisome proliferator-activated receptor gamma, which is a member of the nuclear receptor family and acts as ligand-activated transcription factor of genes involved in glucose metabolism. Herein we present the structure-activity relationships of 16 truxillic acid derivatives, investigated by a cell-based reporter gene assay guided by molecular docking analysis.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding Sites
  • Computer Simulation
  • Cyclobutanes / chemical synthesis
  • Cyclobutanes / chemistry*
  • Cyclobutanes / pharmacology
  • Glucose / metabolism
  • Humans
  • Hypoglycemic Agents / chemical synthesis
  • Hypoglycemic Agents / chemistry*
  • Hypoglycemic Agents / pharmacology
  • PPAR gamma / agonists*
  • PPAR gamma / metabolism
  • Structure-Activity Relationship

Substances

  • Cyclobutanes
  • Hypoglycemic Agents
  • PPAR gamma
  • truxillic acid
  • Glucose