title: Bicyclic piperazinylbenzenesulphonamides are potent and selective 5-HT6 receptor antagonists.
abstract: The synthesis of novel 3-(octahydropyrido[1,2-a]pyrazin-2-yl)- and 3-(hexahydropyrrolo[1,2-a]pyrazin-2-yl)phenyl-2-benzo[b]thiophene sulphonamide derivatives 3, (S)-4 and (R)-4 is described. The compounds show high affinity for the 5-HT6 receptor, excellent selectivity against a range of other receptors and good brain penetration.
authors: Department of Psychiatry, GlaxoSmithKline, New Frontiers Science Park, Third Avenue, Harlow, CM19 5AW, Essex, UK.
authors: Steven M
authors: SM
authors: Bromidge
authors: Stephen E
authors: SE
authors: Clarke
authors: Frank D
authors: FD
authors: King
authors: Peter J
authors: PJ
authors: Lovell
authors: Helen
authors: H
authors: Newman
authors: Graham
authors: G
authors: Riley
authors: Carol
authors: C
authors: Routledge
authors: Halina T
authors: HT
authors: Serafinowska
authors: Douglas R
authors: DR
authors: Smith
authors: David R
authors: DR
authors: Thomas
mesh_terms: D015195:Drug Design; D007700:Kinetics; D008958:Models, Molecular; D008968:Molecular Conformation; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D010879:Piperazines; D011985:Receptors, Serotonin; D012702:Serotonin Antagonists; D013449:Sulfonamides