Potent, selective human beta(3) adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore

Authors
Mathvink, RJ Barritta, AM Candelore, MR Cascieri, MA Deng, LP Tota, L Strader, CD Wyvratt, MJ Fisher, MH Weber, AE
Citation
Rj. Mathvink et al., Potent, selective human beta(3) adrenergic receptor agonists containing a substituted indoline-5-sulfonamide pharmacophore, BIOORG MED, 9(13), 1999, pp. 1869-1874
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
13
Year of publication
1999
Pages
1869 - 1874
Database
ISI
SICI code
0960-894X(19990705)9:13<1869:PSHBAR>2.0.ZU;2-E
Abstract
A series of compounds possessing an N-substituted indoline-5-sulfonamide ph armacophore was prepared and evaluated for their human beta(3) adrenergic r eceptor agonist activity. The SAR of a wide range of urea and heterocyclic substituents is discussed. 4-Octyl thiazole compound 8c was the most potent and selective compound in the series, with 2800-fold selectivity over beta (1) binding and 1400-fold selectivity over beta(2) binding (C) 1999 Elsevie r Science Ltd. All rights reserved.