[Design and synthesis of nitrogen-containing benzoheterocyclic derivatives and their antipsychotic activities]
Shao-Ping Peng1, Lei-Ping Yu, Jian-Qi Li
1Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China.
Abstract:
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.
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