Diphenyl sulfoxides as selective antagonists of the muscarinic M-2 receptor

Authors
Kozlowski, JA Lowe, DB Guzik, HS Zhou, GW Ruperto, VB Duffy, RA McQuade, R Crosby, G Taylor, LA Billard, W Binch, H Lachowicz, JE
Citation
Ja. Kozlowski et al., Diphenyl sulfoxides as selective antagonists of the muscarinic M-2 receptor, BIOORG MED, 10(20), 2000, pp. 2255-2257
Citations number
17
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
20
Year of publication
2000
Pages
2255 - 2257
Database
ISI
SICI code
0960-894X(20001016)10:20<2255:DSASAO>2.0.ZU;2-V
Abstract
Structure-activity studies on [14-(phenylsulfonyl)phenyl] methylpiperazine led to the discovery of 4-cyclohexyl-alpha-[4-[[4- methoxyphenyl](S)-sulfin yl]phenyl]-1-piperazineacetonitrile, 1, an M-2 selective muscarinic antagon ist. Affinity at the cloned human M-2 receptor was 2.7 nM; the M-1/M-2 sele ctivity is 40-fold. (C) 2000 Elsevier Science Ltd. All rights reserved.