title: Novel (4-piperazin-1-ylquinolin-6-yl) arylsulfonamides with high affinity and selectivity for the 5-HT(6) receptor.
abstract: 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.
authors.affiliation: Discovery Chemistry Europe, GlaxoSmithKline, Discovery Research, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK
authors.forename: S M
authors.initials: SM
authors.lastname: Bromidge
authors.forename: K
authors.initials: K
authors.lastname: Griffith
authors.forename: T D
authors.initials: TD
authors.lastname: Heightman
authors.forename: A
authors.initials: A
authors.lastname: Jennings
authors.forename: F D
authors.initials: FD
authors.lastname: King
authors.forename: S F
authors.initials: SF
authors.lastname: Moss
authors.forename: H
authors.initials: H
authors.lastname: Newman
authors.forename: G
authors.initials: G
authors.lastname: Riley
authors.forename: C
authors.initials: C
authors.lastname: Routledge
authors.forename: H T
authors.initials: HT
authors.lastname: Serafinowska
authors.forename: D R
authors.initials: DR
authors.lastname: Thomas
mesh_terms: 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*
chemical_list: D011954:Receptors, Dopamine; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013449:Sulfonamides; C097216:serotonin 6 receptor