5-aryl thiazolidine-2,4-diones: Discovery of PPAR Dual alpha/gamma Agonists as Antidiabetic Agents

Bioorg Med Chem Lett. 2003 Aug 18;13(16):2795-8. doi: 10.1016/s0960-894x(03)00505-5.

Abstract

A novel series of 5-aryl thiazolidine-2,4-diones based dual PPARalpha/gamma agonists was identified. A number of highly potent and orally bioavailable analogues were synthesized. Efficacy study results of some of these analogues in the db/db mice model of type 2 diabetes showed them superior to rosiglitazone in correcting hyperglycemia and hypertriglyceridemia.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy
  • Disease Models, Animal
  • Hyperglycemia / drug therapy
  • Hypertriglyceridemia / drug therapy
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / pharmacology
  • Mice
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Receptors, Cytoplasmic and Nuclear / metabolism
  • Rosiglitazone
  • Structure-Activity Relationship
  • Thiazolidinediones / chemical synthesis*
  • Thiazolidinediones / pharmacology
  • Transcription Factors / agonists*
  • Transcription Factors / metabolism

Substances

  • Hypoglycemic Agents
  • Receptors, Cytoplasmic and Nuclear
  • Thiazolidinediones
  • Transcription Factors
  • Rosiglitazone