| 新的二芳基哌嗪基脒类化合物——化学合成和5-HT重摄取抑制活性 |
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| 引用本文： | 秦芳,王娜沙,杨静,张建军,王亚芳,杨光中.新的二芳基哌嗪基脒类化合物——化学合成和5-HT重摄取抑制活性[J].药学学报,2008,43(6):619-625. |
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| 作者姓名： | 秦芳 王娜沙 杨静 张建军 王亚芳 杨光中 |
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| 作者单位： | 中国医学科学院,北京协和医学院,药物研究所,北京,100050 |
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| 基金项目： | 国家自然科学基金
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北京市自然科学基金 |
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| 摘 要： | 为了寻找新的5-HT重摄取抑制活性的抗抑郁药， 设计合成了31个哌嗪取代的二苯脒类化合物， 通过1H NMR，HRMS对化合物结构进行了确证，并测定了化合物的体外5-HT重摄取抑制活性。结果表明所有化合物都有一定程度的5-HT重摄取抑制活性。其中化合物5i、 4a和5m具有较强的5-HT重摄取抑制活性，其活性与阳性对照品丙咪嗪相当或稍强，值得进一步研究。
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| 关 键 词： | 合成 哌嗪取代的二苯脒类化合物 5-HT重摄取抑制活性 抗抑郁 |
| 文章编号： | 0513-4870(2008)06-0619-07 |
| 收稿时间： | 2007-12-19 |
| 修稿时间： | 2007年12月19 |
Synthesis and 5-HT reuptake inhibition activity of biarylbenzamidine derivatives |
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| QIN Fang,WANG Na-sha,YANG Jing,ZHANG Jian-jun,WANG Ya-fang,YANG Guang-zhong.Synthesis and 5-HT reuptake inhibition activity of biarylbenzamidine derivatives[J].Acta Pharmaceutica Sinica,2008,43(6):619-625. |
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| Authors: | QIN Fang WANG Na-sha YANG Jing ZHANG Jian-jun WANG Ya-fang YANG Guang-zhong |
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| Institution: | Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, Beijing 100050, China. |
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| Abstract: | A series of biarylbenzamidine analogs were synthesized and tested for their biological activities of inhibiting the reuptake of 5-HT. All of them were new compounds, and their structures were confirmed by 1H NMR and HRMS. Preliminary in vitro pharmacological tests showed that all target compounds exhibited 5-HT reuptake inhibition activity. Among the tested compounds, 5i, 4a and 5m exhibited potent inhibitory activity against 5-HT reuptake in vitro. It is a chance to find a better precursor of SSRIs (selective serotonin reuptake inhibitors) for further optimization of compounds. |
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| Keywords: | biarylbenzamidine derivative 5-HT reuptake inhibition activity anti-depression synthesis |
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