Benzylidene ketal derivatives as M-2 muscarinic receptor antagonists

Authors
Boyle, CD Chackalamannil, S Chen, LY Dugar, S Pushpavanam, P Billard, W Binch, H Crosby, G Cohen-Williams, M Coffin, VL Duffy, RA Ruperto, V Lachowicz, JE
Citation
Cd. Boyle et al., Benzylidene ketal derivatives as M-2 muscarinic receptor antagonists, BIOORG MED, 10(24), 2000, pp. 2727-2730
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
24
Year of publication
2000
Pages
2727 - 2730
Database
ISI
SICI code
0960-894X(200012)10:24<2727:BKDAMM>2.0.ZU;2-V
Abstract
Benzylidene ketal derivatives were investigated as selective M-2 receptor a ntagonists for the treatment of Alzheimer's disease. Compound 10 was discov ered to have subnanomolar M-2 receptor affinity and 100-fold selectivity ag ainst other muscarinic receptors. Also, 10 demonstrated in vivo efficacy in rodent models of muscarinic activity and cognition. (C) 2000 Elsevier Scie nce Ltd. All rights reserved.