Synthesis, binding affinity and SAR of new benzolactam derivatives as dopamine D3 receptor ligands

摘要

A series of new benzolactam derivatives was synthesized and the derivatives were evaluated for their/naffinities at the dopamine D1, D2, and D3 receptors. Some of these compounds showed high D2 and/or/nD3 affinity and selectivity over the D1 receptor. The SAR study of these compounds revealed structural/ncharacteristics that decisively influenced their D2 and D3 affinities. Structural models of the complexes/nbetween some of the most representative compounds of this series and the D2 and D3 receptors were/nobtained with the aim of rationalizing the observed experimental results. Moreover, selected compounds/nshowed moderate binding affinity on 5-HT2A which could contribute to reducing the occurrence of extrapyramidal/nside effects as potential antipsychotics.