芳烷醇哌啶类化合物的合成及抗抑郁活性研究  

Synthesis and antidepressant activities of aryl alkanol piperidine derivatives

作　　者：郑永勇[1] 高凯 翁志洁[1] 李建其[1] 

机构地区：[1]上海医药工业研究院创新药物与制药工艺国家重点实验室,上海200040 [2]江苏惠中医药科技有限公司,江苏南京210009

出　　处：《药学学报》2010年第3期324-329,共6页Acta Pharmaceutica Sinica

基　　金：国家自然科学基金资助项目(30772623)

摘　　要：为寻找新型具有抗抑郁活性的单胺递质再摄取抑制剂,设计合成了15个芳烷醇哌啶类未见文献报道的新化合物,结构经1HNMR及HR-MS分析确证。大鼠脑突触体对5-HT、NA和DA再摄取抑制作用体外活性测试结果表明,化合物4、5和8对5-HT、NA和DA再摄取抑制作用较强。小鼠强迫游泳实验发现,化合物4、5和13具有显著的体内抗抑郁效果,化合物4和5值得进一步研究。To explore novel monoamine reuptake inhibitor with antidepressant activity, a series of substituted aryl alkanol piperidine derivatives were designed and synthesized. All of them were new compounds, and their structures were confirmed with 1H NMR and HR-MS. The results showed that compounds 4, 5 and 8 displayed strong 5-HT, NA and DA reuptake inhibiting activities in vitro. Among the tested compounds, 4, 5 and 13 exhibited potent antidepressant activities in the mice forced swimming test. Compounds 4 and 5 have potent antidepressant activities and are worth further development.

关 键 词：芳烷醇哌啶类化合物 单胺递质再摄取抑制剂 合成 抗抑郁活性 

分 类 号：R916[医药卫生—药学]