Synthesis and evaluation of aminomethyl dihydrocinnamates as a new class of PPAR ligands

Bioorg Med Chem Lett. 2006 Dec 15;16(24):6328-33. doi: 10.1016/j.bmcl.2006.09.011. Epub 2006 Sep 26.

Abstract

PPAR ligands with varied subtype selectivity have been synthesized using an achiral aminomethyl dihydrocinnamate template. Several compounds in this series have demonstrated potent plasma glucose and triglyceride lowering capability in rodent models of type 2 diabetes.

MeSH terms

  • Cinnamates / chemical synthesis*
  • Cinnamates / pharmacokinetics*
  • Humans
  • Hypoglycemic Agents / therapeutic use
  • Ligands
  • PPAR alpha / physiology
  • PPAR gamma / physiology
  • Peroxisome Proliferator-Activated Receptors / physiology*
  • Structure-Activity Relationship
  • Thiazolidinediones / chemical synthesis
  • Thiazolidinediones / therapeutic use

Substances

  • Cinnamates
  • Hypoglycemic Agents
  • Ligands
  • PPAR alpha
  • PPAR gamma
  • Peroxisome Proliferator-Activated Receptors
  • Thiazolidinediones