Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta(3) adrenergic receptor agonists

Authors
Parmee, ER Brockunier, LL He, JF Singh, SB Candelore, MR Cascieri, MA Deng, LP Liu, Y Tota, L Wyvratt, MJ Fisher, MH Weber, AE
Citation
Er. Parmee et al., Tetrahydroisoquinoline derivatives containing a benzenesulfonamide moiety as potent, selective human beta(3) adrenergic receptor agonists, BIOORG MED, 10(20), 2000, pp. 2283-2286
Citations number
23
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2283 - 2286
Database
ISI
SICI code
0960-894X(20001016)10:20<2283:TDCABM>2.0.ZU;2-#
Abstract
Tetrahydroisoquinoline derivatives containing a 4-(hexylureido)benzenesulfo namide were examined as human beta (3) adrenergic receptor (AR) agonists. N otably, 4,4-biphenyl derivative 9 was a 6 nM full agonist of the beta (3) A R. Naphthyloxy compound 18 (beta (3) EC50 = 78 nM) did not activate the bet a (1) and beta (2) ARs at 10 muM, and showed >1000-fold selectivity over bi nding to the beta (1) and beta (2) ARs. (C) 2000 Elsevier Science Ltd. All rights reserved.