BMS-201620: a selective beta 3 agonist

Bioorg Med Chem Lett. 2004 Jul 5;14(13):3525-9. doi: 10.1016/j.bmcl.2004.04.074.

Abstract

A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human beta3 adrenergic receptor agonist activity. SAR studies led to the identification of BMS-201620 (39), a potent beta3 full agonist (Ki = 93 nM, 93% activation). Based on its favorable safety profile, BMS-201620 was chosen for clinical evaluation.

Publication types

  • Comparative Study

MeSH terms

  • Adrenergic beta-3 Receptor Agonists*
  • Adrenergic beta-Agonists / chemical synthesis
  • Adrenergic beta-Agonists / pharmacology*
  • Animals
  • Dose-Response Relationship, Drug
  • Drug Evaluation, Preclinical
  • Glycine / analogs & derivatives*
  • Glycine / chemical synthesis
  • Glycine / chemistry
  • Glycine / pharmacology*
  • Haplorhini
  • Humans
  • Methylation
  • Receptors, Adrenergic, beta-3 / metabolism
  • Stereoisomerism
  • Structure-Activity Relationship

Substances

  • Adrenergic beta-3 Receptor Agonists
  • Adrenergic beta-Agonists
  • BMS-201620
  • Receptors, Adrenergic, beta-3
  • glycine amide
  • Glycine