Design and synthesis of a novel class of dual PPARgamma/delta agonists

Bioorg Med Chem Lett. 2007 Feb 15;17(4):1052-5. doi: 10.1016/j.bmcl.2006.11.029. Epub 2006 Nov 15.

Abstract

The design and synthesis of dual PPAR gamma/delta agonist (R)-3-{2-ethyl-4-[3-(4-ethyl-2-pyridin-2-yl-phenoxy)-butoxy]-phenyl}propionic acid is described. This compound dose-dependently lowered plasma glucose in hyperglycemic male Zucker diabetic fatty (ZDF) rats and produced less weight gain relative to rosiglitazone at an equivalent level of glucose control.

Publication types

  • Comparative Study

MeSH terms

  • Animals
  • Blood Glucose / metabolism
  • Dose-Response Relationship, Drug
  • Drug Design
  • Female
  • Half-Life
  • Humans
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / pharmacokinetics
  • Hypoglycemic Agents / pharmacology*
  • Indicators and Reagents
  • Insulin / blood
  • Male
  • PPAR delta / agonists*
  • PPAR gamma / agonists*
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Zucker
  • Rosiglitazone
  • Structure-Activity Relationship
  • Thiazolidinediones / pharmacology
  • Weight Gain / drug effects

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • Indicators and Reagents
  • Insulin
  • PPAR delta
  • PPAR gamma
  • Thiazolidinediones
  • Rosiglitazone