2. Academic Validation
  3. Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists

Synthesis and SAR of aminothiazole fused benzazepines as selective dopamine D2 partial agonists

  • Bioorg Med Chem Lett. 2013 Jan 15;23(2):543-7. doi: 10.1016/j.bmcl.2012.11.023.
Rebecca A Urbanek 1,  Hui Xiong,  Ye Wu,  William Blackwell,  Gary Steelman,  Jim Rosamond,  Steven S Wesolowski,  James B Campbell,  Minli Zhang,  Becky Brockel,  Daniel V Widzowski
Affiliations

Affiliation

  • 1 CNS Discovery, AstraZeneca Pharmaceuticals, 1800 Concord Pike, Wilmington, DE, USA.
PMID: 23237836 DOI: 10.1016/j.bmcl.2012.11.023
Abstract

Dopamine (D(2)) partial agonists (D2PAs) have been regarded as a potential treatment for schizophrenia patients with expected better side effect profiles than currently marketed antipsychotics. Herein we report the synthesis and SAR of a series of aminothiazole fused benzazepines as selective D(2) partial agonists. These compounds have good selectivity, CNS drug-like properties and tunable D(2) partial agonism. One of the key compounds, 8h, has good in vitro/in vivo ADME characteristics, and is active in a rat amphetamine-induced locomotor activity model.

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