Title of article
Synthesis and SAR of benzyl and phenoxymethylene oxadiazole benzenesulfonamides as selective β3 adrenergic receptor agonist antiobesity agents
Author/Authors
Tesfaye Biftu، نويسنده , , Dennis D. Feng، نويسنده , , Gui-Bai Liang، نويسنده , , Howard Kuo، نويسنده , , Xiaoxia Qian، نويسنده , , Elizabeth M. Naylor، نويسنده , , Vincent J. Colandrea، نويسنده , , Mari R. Candelore، نويسنده , , Margaret A. Cascieri، نويسنده , , Lawrence F. ColwellJr.، نويسنده , , Michael J. Forrest، نويسنده , , Gary J. Hom، نويسنده , , D. Euan MacIntyre، نويسنده , , Ralph A. Stearns، نويسنده , , Catherine D. Strader، نويسنده , , Matthew J. Wyvratt Jr.، نويسنده , , Michael H. Fisher، نويسنده , , Ann E. Weber، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2000
Pages
4
From page
1431
To page
1434
Abstract
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 (ED50Gly=0.15 mg/kg). Under these conditions a heart rate increase of 15% was observed at a dose level of 10 mg/kg.
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2000
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
790889
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