title: Dual acting norepinephrine reuptake inhibitors and 5-HT(2A) receptor antagonists: Identification, synthesis and activity of novel 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles.
abstract: The discovery of a series of 4-aminoethyl-3-(phenylsulfonyl)-1H-indoles, dual acting norepinephrine reuptake inhibitors (NRIs) and 5-HT(2A) receptor antagonists, is described. The synthesis and structure-activity relationship (SAR) of this novel series of compounds is also presented.
authors.affiliation: Chemical Sciences, Wyeth Research, 500 Arcola Road, Collegeville, PA 19426, USA. hefferg@wyeth.com
authors.forename: Gavin D
authors.initials: GD
authors.lastname: Heffernan
authors.forename: Richard D
authors.initials: RD
authors.lastname: Coghlan
authors.forename: Eric S
authors.initials: ES
authors.lastname: Manas
authors.forename: Robert E
authors.initials: RE
authors.lastname: McDevitt
authors.forename: Yanfang
authors.initials: Y
authors.lastname: Li
authors.forename: Paige E
authors.initials: PE
authors.lastname: Mahaney
authors.forename: Albert J
authors.initials: AJ
authors.lastname: Robichaud
authors.forename: Christine
authors.initials: C
authors.lastname: Huselton
authors.forename: Peter
authors.initials: P
authors.lastname: Alfinito
authors.forename: Jenifer A
authors.initials: JA
authors.lastname: Bray
authors.forename: Scott A
authors.initials: SA
authors.lastname: Cosmi
authors.forename: Grace H
authors.initials: GH
authors.lastname: Johnston
authors.forename: Thomas
authors.initials: T
authors.lastname: Kenney
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Koury
authors.forename: Richard C
authors.initials: RC
authors.lastname: Winneker
authors.forename: Darlene C
authors.initials: DC
authors.lastname: Deecher
authors.forename: Eugene J
authors.initials: EJ
authors.lastname: Trybulski
mesh_terms: D001692:Biological Transport / Q000187:drug effects; D002460:Cell Line; D006801:Humans; D007211:Indoles / Q000138:chemical synthesis / Q000378:metabolism / Q000494:pharmacology*; D014179:Neurotransmitter Uptake Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D009638:Norepinephrine / Q000378:metabolism*; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D007211:Indoles; D014179:Neurotransmitter Uptake Inhibitors; D044402:Receptor, Serotonin, 5-HT2A; D058830:Serotonin 5-HT2 Receptor Antagonists; D012702:Serotonin Antagonists; D009638:Norepinephrine