Potent, selective 3-pyridylethanolamine beta3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide pharmacophore

Bioorg Med Chem Lett. 2000 Sep 4;10(17):1971-3. doi: 10.1016/s0960-894x(00)00390-5.

Abstract

A series of thiazole benzenesulfonamide-substituted 3-pyridylethanolamines was prepared and evaluated for their human beta3 adrenergic receptor agonist activity. Incorporation of aryl and heteroaryl substitution in the 4-position of the thiazole ring resulted in a number of highly potent and selective beta3 agonists. Results of preliminary in vivo evaluation of several of these compounds is described.

MeSH terms

  • Adrenergic beta-3 Receptor Agonists*
  • Adrenergic beta-Agonists / chemical synthesis*
  • Adrenergic beta-Agonists / pharmacology
  • Animals
  • Benzenesulfonamides
  • CHO Cells
  • Cricetinae
  • Ethanolamines / chemical synthesis*
  • Humans
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis*
  • Thiazoles / chemical synthesis*

Substances

  • Adrenergic beta-3 Receptor Agonists
  • Adrenergic beta-Agonists
  • Ethanolamines
  • Sulfonamides
  • Thiazoles