Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands.
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).
Swain
Christopher J
CJ
The Neuroscience Research Centre, Merck Sharp and Dohme, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK. swain@mac.com <swain@mac.com>
Teran
Ana
A
Maroto
Marta
M
Cabello
Angeles
A
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
D001381:Azepines; D008024:Ligands; D044402:Receptor, Serotonin, 5-HT2A; D006859:Hydrogen