BMS-187257, a potent, selective, and novel heterocyclic β3 adrenergic receptor agonist

• Published in: Bioorganic & medicinal chemistry letters 1996-10, Vol.6 (19), p.2253-2258
• Main Authors: Fisher, Liesl G., Sher, Philip M., Skwish, Stephen, Michel, Inge M., Seiler, Steven M., Dickinson, Kenneth E.J.
• Format: Article
• Language: English
• ISSN: 0960-894X; 1464-3405
• DOI: 10.1016/0960-894X(96)00417-9

Novel heterocyclic β 3 adrenergic receptor agonists 2 were prepared and evaluated for their ability to bind to human β 1, β 2, and β 3 adrenergic receptors. Stimulatory effects on the β 3 adrenergic receptor were also measured. BMS-187257 ( 4b) was found to be a potent and selective β 3 agonist. Novel heterocyclic β 3 adrenergic receptor agonists were prepared and evaluated for their ability to bind to human β 1, β 2, and β 3 adrenergic receptors and to stimulate the β 3 adrenergic receptor. BMS-187257 was found to be a potent and selective β 3 agonist.