308368-70-9Relevant academic research and scientific papers
Potent, selective 3-pyridylethanolamine β3 adrenergic receptor agonists possessing a thiazole benzenesulfonamide
Mathvink, Robert J.,Tolman,Chitty, Dawn,Candelore, Mari R.,Cascieri, Margaret A.,Colwell Jr., Lawrence F.,Deng, Liping,Feeney, William P.,Forrest, Michael J.,Hom, Gary J.,MacIntyre,Tota, Laurie,Wyvratt, Matthew J.,Fisher, Michael H.,Weber, Ann E.
, p. 1971 - 1973 (2007/10/03)
A series of thiazole benzenesulfonamide-substituted 3-pyridylethanolamines was prepared and evaluated for their human β3 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 β3 agonists. Results of preliminary in vivo evaluation of several of these compounds is described. (C) 2000 Elsevier Science Ltd.
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
Mathvink,Hom,MacIntyre,Miller,Stearns,Tota,Wyvratt,Fisher,Weber,Tolman,Chitty,Candelore,Cascieri,Colwell Jr.,Deng,Feeney,Forrest
, p. 3832 - 3836 (2007/10/03)
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.
