Synthesis and SAR of highly potent and selective dopamine D3-receptor antagonists: 1H-Pyrimidin-2-one derivatives

The synthesis and SAR of novel highly potent and selective dopamine D3-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED50 6.1 mg/kg po), a social interaction paradigm.

Graphical abstractThe synthesis and SAR of novel highly potent and selective dopamine D3-receptor antagonists based on a 1H-pyrimidin-2-one scaffold are described. A-690344 antagonized PD 128907-induced huddling deficits in rat (ED50 6.1 mg/kg po), a social interaction paradigm.Figure optionsDownload full-size imageDownload as PowerPoint slide