title: Parallel synthesis of 3-aryloxy-2-propanolamines and evaluation as dual affinity 5-HT(1A) and 5-HT re-uptake ligands.
abstract: A solution phase synthesis for the preparation of 3-aryloxy-2-propanolamine libraries has been developed. This resulted in the identification of 5 as a ligand with dual affinity for 5-HT1A and serotonin reuptake receptors which shows excellent pharmacokinetic parameters.
authors.affiliation: Department of Chemistry, Merck, Sharp & Dohme Research Laboratories, Neuroscience Research Centre, Harlow, Essex, United Kingdom. Monique_vanniel@merck.com
authors.forename: M B
authors.initials: MB
authors.lastname: van Niel
authors.forename: M S
authors.initials: MS
authors.lastname: Beer
authors.forename: J L
authors.initials: JL
authors.lastname: Castro
authors.forename: S K
authors.initials: SK
authors.lastname: Cheng
authors.forename: D C
authors.initials: DC
authors.lastname: Evans
authors.forename: A
authors.initials: A
authors.lastname: Heald
authors.forename: L
authors.initials: L
authors.lastname: Hitzel
authors.forename: P
authors.initials: P
authors.lastname: Hunt
authors.forename: R
authors.initials: R
authors.lastname: Mortishire-Smith
authors.forename: D
authors.initials: D
authors.lastname: O'Connor
authors.forename: A P
authors.initials: AP
authors.lastname: Watt
authors.forename: A M
authors.initials: AM
authors.lastname: MacLeod
mesh_terms: D008024:Ligands; D011412:Propanolamines / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics; D012701:Serotonin / Q000378:metabolism*; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000378:metabolism / Q000493:pharmacokinetics
chemical_list: D008024:Ligands; D011412:Propanolamines; D012701:Serotonin; D017367:Selective Serotonin Reuptake Inhibitors