308368-74-3

Upstream product

• 95727-89-2 4-(trifluoromethyl)phenyl chloromethylketone 
• 211031-93-5 (R)-N-[4-[2-[N-(1,1-dimethylethoxycarbonyl)-N-[2-hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-(aminothiocarbonyl)benzenesulfonamide 
• 49584-26-1 p-cyanobenzenesulfonyl chloride 
• 173901-05-8 (R)-N-[2-(4-aminophenyl)ethyl]-2-hydroxy-2-(3-pyridyl)ethylcarbamic acid 1,1-dimethylethyl ester 
• 182251-98-5 (R)-N-[4-[2-[N-(1,1-Dimethylethoxycarbonyl)-N-[2-Hydroxy-2-(Pyridin-3-Yl)ethyl]Amino]Ethyl]Phenyl]-4-Cyano-Benzensulfonamide 

Relevant academic research and scientific papers

Discovery of a potent, orally bioavailable β3 adrenergic receptor agonist, (R)-N-[4-[2-[[2-Hydroxy-2-(3-pyridinyl)ethyl]amino]ethyl]phenyl]-4-[4-[4-(tri fluoromethyl)phenyl]thiazol-2-yl]benzenesulfonamide

As part of our investigation into the development of orally bioavailable β3 adrenergic receptor agonists, we have identified a series of pyridylethanolamine analogues possessing a substituted thiazole benzenesulfonamide pharmacophore that are potent human β3 agonists with excellent selectivity against other human β receptor subtypes. Several of these compounds also exhibited an improved pharmacokinetic profile in dogs. For example, thiazole sulfonamide 2e (R = 4-F3C-C6H4) is a potent full β3 agonist (EC50 = 3.6 nM, 94% activation) with >600-fold selectivity over the human β1 and β2 receptors, which also displays good oral bioavailability in several mammalian species, as well as an extended duration of action.