5-Aryl thiazolidine-2,4-diones as selective PPARgamma agonists

Bioorg Med Chem Lett. 2003 May 19;13(10):1801-4. doi: 10.1016/s0960-894x(03)00257-9.

Abstract

A series of 5-aryl thiazolidine-2,4-diones containing 4-phenoxyphenyl side chains was designed, synthesized, and evaluated for PPAR agonist activities. One such compound 28 exhibited comparable levels of glucose correction to rosiglitazone in the db/db mouse type 2 diabetes animal model.

MeSH terms

  • Animals
  • Blood Glucose / drug effects
  • Diabetes Mellitus, Type 2 / drug therapy
  • Disease Models, Animal
  • Hypoglycemic Agents / chemical synthesis*
  • Hypoglycemic Agents / pharmacokinetics
  • Hypoglycemic Agents / pharmacology
  • Inhibitory Concentration 50
  • Mice
  • Receptors, Cytoplasmic and Nuclear / agonists*
  • Structure-Activity Relationship
  • Thiazolidinediones / chemical synthesis*
  • Thiazolidinediones / pharmacokinetics*
  • Thiazolidinediones / pharmacology
  • Transcription Factors / agonists*

Substances

  • Blood Glucose
  • Hypoglycemic Agents
  • Receptors, Cytoplasmic and Nuclear
  • Thiazolidinediones
  • Transcription Factors
  • 2,4-thiazolidinedione