Synthesis and SAR of highly potent and selective dopamine D(3)-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives. [email protected]

Bioorg Med Chem Lett. 2006 Feb;16(3):658-62. doi: 10.1016/j.bmcl.2005.10.035. Epub 2005 Nov 2.

Abstract

The synthesis and SAR of novel and selective dopamine D(3)-receptor antagonists based on a 3,4-dihydro-1H-quinolin-2-one, a 1,3,4,5-tetrahydro-benzo[b]azepin-2-one, 1H-quinoline-2,4-dione or a 3,4-dihydro-1H-benzo[b]azepine-2,5-dione scaffold are discussed. A706149 (2.15mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigm.

MeSH terms

  • Animals
  • Benzazepines / chemical synthesis*
  • Benzazepines / pharmacology
  • Dopamine Antagonists / chemical synthesis*
  • Dopamine Antagonists / pharmacology
  • Models, Molecular
  • Molecular Structure
  • Quinolones / chemical synthesis*
  • Quinolones / pharmacology
  • Rats
  • Receptors, Dopamine D3 / antagonists & inhibitors*
  • Structure-Activity Relationship

Substances

  • Benzazepines
  • Dopamine Antagonists
  • Quinolones
  • Receptors, Dopamine D3