Discovery of an orally bioavailable alkyl oxadiazole beta(3) adrenergic receptor agonist

Authors
Feng, DQD Biftu, T Candelore, MR Cascieri, MA Colwell, LF Deng, LP Feeney, WP Forrest, MJ Hom, GJ MacIntyre, DE Miller, RR Stearns, RA Strader, CD Tota, L Wyvratt, MJ Fisher, MH Weber, AE
Citation
Dqd. Feng et al., Discovery of an orally bioavailable alkyl oxadiazole beta(3) adrenergic receptor agonist, BIOORG MED, 10(13), 2000, pp. 1427-1429
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
13
Year of publication
2000
Pages
1427 - 1429
Database
ISI
SICI code
0960-894X(20000703)10:13<1427:DOAOBA>2.0.ZU;2-C
Abstract
5-n-Pentyl oxadiazole substituted benzenesulfonamide 8 is a potent and sele ctive beta(3) adrenergic receptor agonist (beta(3) EC50 = 23 nM, beta(1) IC 50 = 3000 nM, beta(2) IC50 = 3000 nM). The compound has high oral bioavaila bility in dogs (62%) and rats (36%) and is among the: most orally bioavaila ble beta(3) adrenergic receptor agonists reported to date. (C) 2000 Elsevie r Science Ltd. All rights reserved.