Design and synthesis of novel PPARalpha/gamma/delta triple activators using a known PPARalpha/gamma dual activator as structural template

Bioorg Med Chem Lett. 2003 Jan 20;13(2):257-60. doi: 10.1016/s0960-894x(02)00881-8.


Using a known dual PPARalpha/gamma activator (5) as a structural template, SAR evaluations led to the identification of triple PPARalpha/gamma/delta activators (18-20) with equal potency and efficacy on all three receptors. These compounds could become useful tools for studying the combined biological effects of PPARalpha/gamma/delta activation.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Blood Glucose / metabolism
  • Glucose Tolerance Test
  • Insulin / blood
  • Male
  • Mice
  • Models, Molecular
  • Molecular Conformation
  • Receptors, Cytoplasmic and Nuclear / chemistry
  • Receptors, Cytoplasmic and Nuclear / drug effects*
  • Structure-Activity Relationship
  • Transcription Factors / chemistry
  • Transcription Factors / drug effects*


  • Blood Glucose
  • Insulin
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors