title: Novel pyridyl-fused 3-amino chroman derivatives with dual action at serotonin transporter and 5-HT1A receptor.
abstract: Structural modifications of the initial lead, 3-aminochroman (4), led to the identification of a novel series of pyridyl-fused amino chroman derivatives (5-8) and the structural isomers (9-12). The compounds described were evaluated for dual 5-HT transporter inhibitory and 5-HT(1A) receptor activities. The design strategy, synthesis, and in vitro biological characterization for these novel compounds are described.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543-8000, USA. zhoud@wyeth.com
authors.forename: Dahui
authors.initials: D
authors.lastname: Zhou
authors.forename: Nicole T
authors.initials: NT
authors.lastname: Hatzenbuhler
authors.forename: Jonathan L
authors.initials: JL
authors.lastname: Gross
authors.forename: Boyd L
authors.initials: BL
authors.lastname: Harrison
authors.forename: Deborah A
authors.initials: DA
authors.lastname: Evrard
authors.forename: Michael
authors.initials: M
authors.lastname: Chlenov
authors.forename: Jeannette
authors.initials: J
authors.lastname: Golembieski
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Hornby
authors.forename: Lee E
authors.initials: LE
authors.lastname: Schechter
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Smith
authors.forename: Terrance H
authors.initials: TH
authors.lastname: Andree
authors.forename: Gary P
authors.initials: GP
authors.lastname: Stack
mesh_terms: D000818:Animals; D002839:Chromans / Q000737:chemistry* / Q000494:pharmacology*; D006801:Humans; D051381:Rats; D044282:Receptor, Serotonin, 5-HT1A / Q000187:drug effects* / Q000378:metabolism; D050486:Serotonin Plasma Membrane Transport Proteins / Q000187:drug effects* / Q000378:metabolism; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*
chemical_list: D002839:Chromans; D044282:Receptor, Serotonin, 5-HT1A; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors