title: Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.
abstract: A several series of low molecular weight 5-HT(2A) leads were identified from an analysis of HTS data, the exploration of SAR and optimization of one series using parallel synthesis are described, affording compound 22 (5-HT(2A) IC(50) 1.1 nM).
authors.affiliation: The Neuroscience Research Centre, Merck Sharp and Dohme, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK. swain@mac.com <swain@mac.com>
authors.forename: Christopher J
authors.initials: CJ
authors.lastname: Swain
authors.forename: Ana
authors.initials: A
authors.lastname: Teran
authors.forename: Marta
authors.initials: M
authors.lastname: Maroto
authors.forename: Angeles
authors.initials: A
authors.lastname: Cabello
mesh_terms: D000586:Amination; D001381:Azepines / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism*; D006801:Humans; D006859:Hydrogen / Q000737:chemistry*; D008024:Ligands; D015394:Molecular Structure; D044402:Receptor, Serotonin, 5-HT2A / Q000378:metabolism*; D013329:Structure-Activity Relationship
chemical_list: D001381:Azepines; D008024:Ligands; D044402:Receptor, Serotonin, 5-HT2A; D006859:Hydrogen