药学学报, 2014, 49(10): 1442-1445
引用本文:
范於菟, 武祥龙, 潘亚磊, 牛银波, 李晨睿, 梅其炳. 新型苯甲酰胺类化合物的合成与抗疲劳活性研究[J]. 药学学报, 2014, 49(10): 1442-1445.
FAN Wu-tu, WU Xiang-long, PAN Ya-lei, NIU Yin-bo, LI Chen-rui, MEI Qi-bing. Synthesis and antifatigue activities of new benzamide derivatives[J]. Acta Pharmaceutica Sinica, 2014, 49(10): 1442-1445.

新型苯甲酰胺类化合物的合成与抗疲劳活性研究
范於菟1, 武祥龙2, 潘亚磊2, 牛银波2, 李晨睿2, 梅其炳2,3
1. 三峡大学生物与制药学院, 天然产物研究与利用湖北省重点实验室, 湖北 宜昌 443002;
2. 西北工业大学生命学院, 空间生物实验模拟技术国防重点学科实验室, 陕西 西安 710072;
3. 第四军医大学药学院药理教研室, 陕西 西安 710032
摘要:
为寻找以AMPA受体为作用靶点的新型抗疲劳化合物,以1-(1,3-benzodioxol-5-ylcarbonyl)piperidine(1-BCP)为先导化合物,设计合成了10个新化合物,结构经1H NMR、ESI-MS及元素分析确证。采用小鼠负重游泳实验评价目标化合物抗疲劳活性,采用放射性配体受体结合实验测定化合物与AMPA受体的亲和力。结果表明,化合物5b具有显著的抗疲劳活性,且与AMPA受体的亲和力较强,值得进一步深入研究。
关键词:    苯甲酰胺类化合物      合成      疲劳      AMPA受体     
Synthesis and antifatigue activities of new benzamide derivatives
FAN Wu-tu1, WU Xiang-long2, PAN Ya-lei2, NIU Yin-bo2, LI Chen-rui2, MEI Qi-bing2,3
1. Hubei Key Laboratory of Natural Products Research and Development, College of Biology and Pharmacy, China Three Gorges University, Yichang 443002, China;
2. Key Laboratory for Space Biosciences and Biotechnology, School of Life Sciences, Northwestern Polytechnical University, Xi'an 710072, China;
3. Department of Pharmacology, School of Pharmacy, Fourth Military Medical University, Xi'an 710032, China
Abstract:
To explore novel antifatigue agents targeting with AMPA receptor, 10 compounds were synthesized and their structures were confirmed by 1H NMR, ESI-MS and elemental analysis. 1-BCP was treated as the leading compound. The antifatigue activities were evaluated by weight-loaded forced swimming test, and the AMPA receptor binding affinities were tested with radioligand receptor binding assays. The results unveiled that 5b appeared to possess potent antifatigue activities and high affinity with AMPA receptor, which deserved further studies.
Key words:    benzamides    synthesis    fatigue    AMPA receptor   
收稿日期: 2014-05-04
基金项目: 国家“重大新药创制”科技重大专项(2008ZXJ09004-024);国家自然科学基金资助项目(21202130)
通讯作者: 梅其炳,Tel/Fax:86-29-88460543,E-mail:qbmei@nwpu.edu.cn
Email: qbmei@nwpu.edu.cn
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