Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors

Authors
Novelli, F Sparatore, A Tasso, B Sparatore, F
Citation
F. Novelli et al., Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors, BIOORG MED, 9(20), 1999, pp. 3031-3034
Citations number
13
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
9
Issue
20
Year of publication
1999
Pages
3031 - 3034
Database
ISI
SICI code
0960-894X(19991018)9:20<3031:QDO5>2.0.ZU;2-0
Abstract
Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzep ine and nuvenzepine, were prepared and tested as ligands for muscarinic M-1 , M-2 and M-3 receptors; 5,11-dihydro-11-[(S-lupinyl)-thioacetyl]-6H-pyrido [2,3-b][1,4]benzodiazepin-6-one exhibited IC50 = 10 nM for M-1 and 760 nM f or both M2 and M3 subtypes. During the synthesis some interesting side comp ounds were isolated and characterized. (C) 1999 Elsevier Science Ltd. All r ights reserved.