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

Bioorg Med Chem Lett

The Neuroscience Research Centre, Merck Sharp and Dohme, Terlings Park, Eastwick Road, Harlow, Essex, CM20 2QR, UK.

Published: December 2006

AI Article Synopsis

  • Researchers identified a series of low molecular weight compounds that target the 5-HT(2A) receptor through high-throughput screening (HTS) data analysis.
  • They explored structure-activity relationships (SAR) to understand how different chemical structures affect the activity of these compounds.
  • The optimization process involved parallel synthesis, leading to the development of compound 22, which demonstrated a strong inhibitory concentration (IC(50) of 1.1 nM) against the 5-HT(2A) receptor.

Article 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).

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http://dx.doi.org/10.1016/j.bmcl.2006.08.108DOI Listing

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