2,4-Thiazolidinediones as potent and selective human beta3 agonists

Bioorg Med Chem Lett. 2001 Mar 26;11(6):757-60. doi: 10.1016/s0960-894x(01)00063-4.

Abstract

Methylsulfonamide substituted 2,4-thiazolidinedione 22c is a potent (EC50=0.01 microM, IA=1.19) and selective (more than 110-fold over beta1 and beta2 agonist activity) beta3 agonist. This compound has also been proven to be active and selective in an in vivo mode.

MeSH terms

  • Adrenergic beta-3 Receptor Agonists*
  • Animals
  • Diabetes Mellitus, Type 2 / drug therapy
  • Disease Models, Animal
  • Humans
  • Mice
  • Mice, Knockout
  • Mice, Transgenic
  • Obesity / drug therapy
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis
  • Thiazoles / chemistry
  • Thiazoles / pharmacology*
  • Thiazoles / therapeutic use
  • Thiazolidinediones*

Substances

  • Adrenergic beta-3 Receptor Agonists
  • Thiazoles
  • Thiazolidinediones
  • 2,4-thiazolidinedione