293306-83-9Relevant articles and documents
Substituted oxazole benzenesulfonamides as potent human β3 adrenergic receptor agonists
Ok,Reigle,Candelore,Cascieri,Colwell,Deng,Feeney,Forrest,Hom,MacIntyre,Strader,Tota,Wang,Wyvratt,Fisher,Weber
, p. 1531 - 1534 (2000)
As a part of our investigation into the development of orally bioavailable β3 adrenergic receptor agonists, we have identified a series of substituted oxazole derivatives that are potent β3 agonists with excellent selectivity against other β receptors. Several of these compounds showed excellent oral bioavailability in dogs. One example, cyclopentylethyloxazole 5f is a potent β3 agonist (EC50 = 14 nM, 84% activation) with 340-fold and 160-fold selectivity over β1 and β2 receptors, respectively, and has 38% oral bioavailability in dogs. (C) 2000 Elsevier Science Ltd. All rights reserved.