New fused benzazepine as selective D3 receptor antagonists. Synthesis and biological evaluation. Part one: [h]-fused tricyclic systems

The synthesis and SAR of a new series of potent and selective dopamine D3 receptor antagonists is reported. The introduction of a tricyclic [h]-fused benzazepine moiety on the recently disclosed scaffold of 1,2,4-triazol-3-yl-thiopropyl-tetrahydrobenzazepines is reported. A full rat pharmacokinetic characterization is also reported.

Graphical abstractThe synthesis of a new class of potent and selective D3 antagonists is reported.Figure optionsDownload full-size imageDownload as PowerPoint slide