Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT6 receptor

Authors
Bromidge, SM Griffith, K Heightman, TD Jennings, A King, FD Moss, SF Newman, H Riley, G Routledge, C Serafinowska, HT Thomas, DR
Citation
Sm. Bromidge et al., Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT6 receptor, BIOORG MED, 11(21), 2001, pp. 2843-2846
Citations number
14
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
11
Issue
21
Year of publication
2001
Pages
2843 - 2846
Database
ISI
SICI code
0960-894X(20011105)11:21<2843:N(AWHA>2.0.ZU;2-D
Abstract
The discovery of (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides and their binding affinites for a selection of 5-HT and dopamine subreceptors is des cribed. Many compounds show high afffinity (pK(i) > 8) for the 5-HT6 recept or and > 100-fold selectivity against a range of other receptors. Structure -activity relationships of these compounds are discussed. (C) 2001 Elsevier Science Ltd. All rights reserved.