Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: Quinolin(di)one and benzazepin(di)one derivatives

The synthesis and SAR of novel and selective dopamine D3-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 (2.15 mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigm.

Graphical abstractThe synthesis and SAR of novel and selective dopamine D3-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. A-706149 (2.15 mg/kg, po) antagonizes PD 128907-induced huddling deficits in rat, a social interaction paradigmFigure optionsDownload full-size imageDownload as PowerPoint slide