Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
The discovery of (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides and their binding affinities for a selection of 5-HT and dopamine subreceptors is described. Many compounds show high affinity (pK(i)>8) for the 5-HT(6) receptor and >100-fold selectivity against a range of other receptors. Structure-activity relationships of these compounds are discussed.
Bromidge
S M
SM
Discovery Chemistry Europe, GlaxoSmithKline, Discovery Research, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK
Griffith
K
K
Heightman
T D
TD
Jennings
A
A
King
F D
FD
Moss
S F
SF
Newman
H
H
Riley
G
G
Routledge
C
C
Serafinowska
H T
HT
Thomas
D R
DR
D015394:Molecular Structure; D011954:Receptors, Dopamine / Q000187:drug effects; D011985:Receptors, Serotonin / Q000187:drug effects*; D012702:Serotonin Antagonists / Q000737:chemistry / Q000494:pharmacology*; D013449:Sulfonamides / Q000737:chemistry / Q000494:pharmacology*
D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013449:Sulfonamides; C097216:serotonin 6 receptor