294843-46-2Relevant academic research and scientific papers
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective β3 adrenergic receptor agonist antiobesity agents
Biftu, Tesfaye,Feng, Dennis D.,Liang, Gui-Bai,Kuo, Howard,Qian, Xiaoxia,Naylor, Elizabeth M.,Colandrea, Vincent J.,Candelore, Mari R.,Cascieri, Margaret A.,Colwell Jr., Lawrence F.,Forrest, Michael J.,Hom, Gary J.,MacIntyre, D. Euan,Stearns, Ralph A.,Strader, Catherine D.,Wyvratt, Matthew J.,Fisher, Michael H.,Weber, Ann E.
, p. 1431 - 1434 (2000)
Benzyl and phenoxymethylene substituted oxadiazoles are potent and orally bioavailable β3 adrenergic receptor (AR) agonists. The 4-trifluormethoxy substituted 5-benzyl oxadiazole 5f has an EC50 of 8 nM in the β3 AR agonist assay with 100-fold selectivity over β1 and β2 AR binding inhibition activity. Its oral bioavailability in dogs is 30 ± 4%, with a half-life of 3.8 ± 0.4 h. In the anesthetized rhesus, 5f evoked a dose-dependent glycerolemia (ED(50Gly) = 0.15 mg/kg). Under these conditions a heart rate increase of 15% was observed at a dose level of 10 mg/kg. (C) 2000 Published by Elsevier Science Ltd. All rights reserved.
