Design and synthesis of highly potent and selective human peroxisome proliferator-activated receptor alpha agonists

Bioorg Med Chem Lett. 2007 Aug 15;17(16):4689-93. doi: 10.1016/j.bmcl.2007.05.066. Epub 2007 May 24.

Abstract

A combination of benzoxazole, phenoxyalkyl side chain, and phenoxybutyric acids was identified as a highly potent and selective human peroxisome proliferator-activated receptor alpha (PPARalpha) agonist. The synthesis, structure-activity relationship (SAR) studies, and in vivo activities of the representative compounds are described.

MeSH terms

  • Allergens
  • Animals
  • Antigens, Plant
  • Drug Design
  • Heterocyclic Compounds / chemistry*
  • Heterocyclic Compounds / pharmacology*
  • Humans
  • Hypolipidemic Agents / chemistry
  • Hypolipidemic Agents / pharmacology
  • Mice
  • Mice, Transgenic
  • Molecular Structure
  • PPAR alpha / agonists*
  • Plant Proteins
  • Rats
  • Rats, Sprague-Dawley
  • Structure-Activity Relationship

Substances

  • Allergens
  • Antigens, Plant
  • Heterocyclic Compounds
  • Hypolipidemic Agents
  • MALD1 protein, Malus domestica
  • PPAR alpha
  • Plant Proteins