293306-72-6Relevant articles and documents
1,3-Oxazole-based selective picomolar inhibitors of cytosolic human carbonic anhydrase II alleviate ocular hypertension in rabbits: Potency is supported by X-ray crystallography of two leads
Ferraroni, Marta,Lucarini, Laura,Masini, Emanuela,Korsakov, Mikhail,Scozzafava, Andrea,Supuran, Claudiu T.,Krasavin, Mikhail
, p. 4560 - 4565 (2017/10/06)
Two lead 1,3-oxazole-based carbonic anhydrase inhibitors (CAIs) earlier identified as selective, picomolar inhibitors of hCA II (a cytosolic target for treatment of glaucoma) have been investigated further. Firstly, they were found to be conveniently synt
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 (2007/10/03)
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.