Design, synthesis and evaluation of substituted phenylpropanoic acid derivatives as peroxisome proliferator-activated receptor (PPAR) activators: novel human PPARalpha-selective activators

Bioorg Med Chem Lett. 2002 Jan 7;12(1):77-80. doi: 10.1016/s0960-894x(01)00672-2.

Abstract

A series of substituted phenylpropanoic acid derivatives was prepared as part of a search for subtype-selective human peroxisome proliferator-activated receptor (PPAR) activators. Structure-activity relationship studies indicated that the substituent at the alpha-position of the carboxyl group plays a key role in determining the potency and the selectivity for PPAR transactivation.

MeSH terms

  • Animals
  • COS Cells
  • Drug Design
  • Drug Evaluation, Preclinical
  • Genes, Reporter
  • Humans
  • Phenylpropionates / chemical synthesis*
  • Phenylpropionates / chemistry
  • Phenylpropionates / pharmacology*
  • Protein Isoforms / agonists
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Structure-Activity Relationship
  • Transcription Factors / agonists*
  • Transcriptional Activation / drug effects
  • Transfection

Substances

  • Phenylpropionates
  • Protein Isoforms
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors