Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands

Christopher J Swain; Ana Teran; Marta Maroto; Angeles Cabello

doi:10.1016/j.bmcl.2006.08.108

Identification and optimisation of 5-amino-7-aryldihydro-1,4-diazepines as 5-HT2A ligands

Bioorg Med Chem Lett. 2006 Dec 1;16(23):6058-62. doi: 10.1016/j.bmcl.2006.08.108. Epub 2006 Sep 12.

Authors

Christopher J Swain¹, Ana Teran, Marta Maroto, Angeles Cabello

Affiliation

¹ The Neuroscience Research Centre, Merck Sharp and Dohme, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK. swain@mac.com <swain@mac.com>

PMID: 16971119
DOI: 10.1016/j.bmcl.2006.08.108

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).

MeSH terms

Amination
Azepines / chemical synthesis
Azepines / chemistry*
Azepines / metabolism*
Humans
Hydrogen / chemistry*
Ligands
Molecular Structure
Receptor, Serotonin, 5-HT2A / metabolism*
Structure-Activity Relationship

Substances

Azepines
Ligands
Receptor, Serotonin, 5-HT2A
Hydrogen