Human beta 3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides

Authors
Brockunier, LL Parmee, ER Ok, HO Candelore, MR Cascieri, MA Colwell, LF Deng, LP Feeney, WP Forrest, MJ Hom, GJ MacIntyre, DE Tota, L Wyvratt, MJ Fisher, MH Weber, AE
Citation
Ll. Brockunier et al., Human beta 3-adrenergic receptor agonists containing 1,2,3-triazole-substituted benzenesulfonamides, BIOORG MED, 10(18), 2000, pp. 2111-2114
Citations number
18
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
18
Year of publication
2000
Pages
2111 - 2114
Database
ISI
SICI code
0960-894X(20000918)10:18<2111:HB3RAC>2.0.ZU;2-C
Abstract
Compounds containing a 1,2,3-triazole-substituted benzenesulfonamide were p repared and found to be potent and selective human beta(3)-adrenergic recep tor agonists. The most interesting compound, trifluoromethylbenzyl analogue 12e (beta(3) EC50 = 3.1 nM with >1500-fold selectivity over binding to bot h beta(1)- and beta(2) receptors), stimulates lipolysis in the rhesus monke y (ED50 = 0.36 mg/kg) and is 25% orally bioavailable in the dog. (C) 2000 E lsevier Science Ltd. All rights reserved.