title: Synthesis and structure-activity relationship of novel lactam-fused chroman derivatives having dual affinity at the 5-HT(1A) receptor and the serotonin transporter.
abstract: The structure-activity relationship (SAR) for three series of lactam-fused chroman derivatives possessing 3-amino substituents was evaluated. Many compounds exhibited affinities for both the 5-HT(1A) receptor and the 5-HT transporter. Compounds 45 and 53 demonstrated 5-HT(1A) antagonist activities in the in vitro cAMP turnover model.
authors.affiliation: Chemical and Screening Sciences, Wyeth Research, CN 8000, Princeton, NJ 08543, United States. shenz@wyeth.com
authors.forename: Zhongqi
authors.initials: Z
authors.lastname: Shen
authors.forename: P
authors.initials: P
authors.lastname: Siva Ramamoorthy
authors.forename: Nicole T
authors.initials: NT
authors.lastname: Hatzenbuhler
authors.forename: Deborah A
authors.initials: DA
authors.lastname: Evrard
authors.forename: Wayne
authors.initials: W
authors.lastname: Childers
authors.forename: Boyd L
authors.initials: BL
authors.lastname: Harrison
authors.forename: Michael
authors.initials: M
authors.lastname: Chlenov
authors.forename: Geoffrey
authors.initials: G
authors.lastname: Hornby
authors.forename: Deborah L
authors.initials: DL
authors.lastname: Smith
authors.forename: Kelly M
authors.initials: KM
authors.lastname: Sullivan
authors.forename: Lee E
authors.initials: LE
authors.lastname: Schechter
authors.forename: Terrance H
authors.initials: TH
authors.lastname: Andree
mesh_terms: D002839:Chromans / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D000242:Cyclic AMP / Q000378:metabolism; D015195:Drug Design; D007769:Lactams / Q000737:chemistry*; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism; D058829:Serotonin 5-HT1 Receptor Antagonists; D050486:Serotonin Plasma Membrane Transport Proteins / Q000737:chemistry / Q000378:metabolism*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
chemical_list: D002839:Chromans; D000242:Cyclic AMP; D007769:Lactams; D044282:Receptor, Serotonin, 5-HT1A; D058829:Serotonin 5-HT1 Receptor Antagonists; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors