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。
To explore novel antifatigue agents targeting with AMPA receptor, 10 compounds were synthesized and their structures were confirmed by lH 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.
出处
《药学学报》
CAS
CSCD
北大核心
2014年第10期1442-1445,共4页
Acta Pharmaceutica Sinica
基金
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)
