Selective PPARgamma modulators with improved pharmacological profiles

Bioorg Med Chem Lett. 2005 May 16;15(10):2437-40. doi: 10.1016/j.bmcl.2005.03.092.

Abstract

A series of metabolically robust N-benzyl-indole selective PPARgamma modulators with either a 3-benzoyl or 3-benzisoxazoyl moiety have been identified. In vitro, these compounds are partial agonists and exhibit reduced adipogenesis in human adipocytes. In vivo, these SPPARgammaMs result in potent glucose lowering in db/db mice and attenuate increases in heart weight and brown adipose tissue that is typically observed in rats upon treatment with PPARgamma full agonists.

MeSH terms

  • Animals
  • Area Under Curve
  • Blood Glucose / metabolism
  • Humans
  • Indoles / chemistry
  • Indoles / pharmacokinetics
  • Indoles / pharmacology*
  • Mice
  • PPAR gamma / drug effects*
  • Rats

Substances

  • Blood Glucose
  • Indoles
  • PPAR gamma