Aryloxazolidinediones: identification of potent orally active PPAR dual alpha/gamma agonists

Bioorg Med Chem Lett. 2003 Oct 20;13(20):3541-4. doi: 10.1016/s0960-894x(03)00785-6.

Abstract

A series of novel aryloxazolidine-2,4-diones was synthesized. A structure-activity relationship study of these compounds led to the identification of potent, orally active PPAR dual alpha/gamma agonists. Based on the results of efficacy studies in the db/db mice model of type 2 diabetes and the desired pharmacokinetic parameters, compound 12 was selected for further profiling.

MeSH terms

  • Administration, Oral
  • Hypoglycemic Agents / chemistry
  • Hypoglycemic Agents / pharmacokinetics
  • Hypoglycemic Agents / pharmacology*
  • Oxazoles / chemistry
  • Oxazoles / pharmacokinetics
  • Oxazoles / pharmacology*
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Structure-Activity Relationship
  • Transcription Factors / agonists*

Substances

  • Hypoglycemic Agents
  • Oxazoles
  • Receptors, Cytoplasmic and Nuclear
  • Transcription Factors