Human beta(3) adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties

Authors
Brockunier, LL Candelore, MR Cascieri, MA Liu, Y Tota, L Wyvratt, MJ Fisher, MH Weber, AE Parmee, ER
Citation
Ll. Brockunier et al., Human beta(3) adrenergic receptor agonists containing cyanoguanidine and nitroethylenediamine moieties, BIOORG MED, 11(3), 2001, pp. 379-382
Citations number
15
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
3
Year of publication
2001
Pages
379 - 382
Database
ISI
SICI code
0960-894X(20010212)11:3<379:HBARAC>2.0.ZU;2-5
Abstract
Pyridineethanolamine derivatives containing cyanoguanidine or nitroethylene diamine moieties were examined as human Bi adrenergic receptor (AR) agonist s. Notably, indoline derivatives 6a and 11 were potent beta (3) AR agonists (beta (3) EC50 = 13 and 19 nM, respectively), which showed good selectivit y over binding to and minimal activation of the beta (1) and beta (2) ARs. (C) 2001 Elsevier Science Ltd. All rights reserved.