O-arylmandelic acids as highly selective human PPAR alpha/gamma agonists

Bioorg Med Chem Lett. 2003 Oct 6;13(19):3185-90. doi: 10.1016/s0960-894x(03)00702-9.

Abstract

A new class of O-arylmandelic acid PPAR agonists show excellent anti-hyperglycemic efficacy in a db/db mouse model of DM2. These PPARalpha-weighted agonists do not show the typical PPARgamma associated side effects of BAT proliferation and cardiac hypertrophy in a rat tolerability assay.

MeSH terms

  • Animals
  • Mandelic Acids / metabolism
  • Mandelic Acids / pharmacology*
  • Mice
  • Mice, Inbred C57BL
  • Mice, Transgenic
  • Protein Binding / drug effects
  • Protein Binding / physiology
  • Rats
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Transcription Factors / agonists*
  • Transcription Factors / metabolism

Substances

  • Mandelic Acids
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors