Design and synthesis of nitrogen-containing benzoheterocyclic derivatives and their antipsychotic activities

A series of nitrogen-containing benzoheterocyclic derivatives were synthesized and tested for  their antipsychotic activities.  Their structures were confirmed by ¹H NMR and HR-MS.  Preliminary in vitro pharmacological trials showed that most of the target compounds have high affinity with D₂ and 5-HT_2A receptors.  Among the tested compounds, 20 exhibited the highest affinity and D₂ partial agonist activity.  In vivo studies showed 20 has potent antipsychotic activities on apomorphine mice model, which is a chance to find a better precursor of D₂ partial agonist for further optimization.