Diphenylsulfone muscarinic antagonists: Piperidine derivatives with high M-2 selectivity and improved potency

Authors
Billard, W Binch, H Bratzler, K Chen, LY Crosby, G Duffy, RA Dugar, S Lachowicz, J McQuade, R Pushpavanam, P Ruperto, VB Taylor, LA Clader, JW
Citation
W. Billard et al., Diphenylsulfone muscarinic antagonists: Piperidine derivatives with high M-2 selectivity and improved potency, BIOORG MED, 10(19), 2000, pp. 2209-2212
Citations number
10
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
19
Year of publication
2000
Pages
2209 - 2212
Database
ISI
SICI code
0960-894X(20001002)10:19<2209:DMAPDW>2.0.ZU;2-T
Abstract
Piperidine analogues of our previously described piperazine muscarinic anta gonists are described. Piperidine analogues show a distinct structure-activ ity relationship (SAR) that differs from comparable piperazines. Compounds with high selectivity and improved potency for the M-2 receptor have been i dentified. The lead compound, 12b, increases acetylcholine release in vivo. Compounds of this class may be useful for the treatment of cognitive disor ders such as Alzheimer's disease (AD). (C) 2000 Elsevier Science Ltd. All r ights reserved.