用原位点击化学方法合成新型乙酰胆碱抑制剂  

Synthesis of the novel acetylcholinesterase inhibitors by in situ click chemistry

作　　者：郭永彪[1] 刘海波[1] 许明[1] 

机构地区：[1]防化研究院,北京102205

出　　处：《现代仪器》2012年第3期43-46,共4页Modern Instruments

摘　　要：采用高效液相色谱-质谱联用技术,分析加入叠氮和炔构建块的乙酰胆碱酯酶(AChE)孵育液。找到4个乙酰胆碱酯酶诱导叠氮和炔构建块发生Husigen[3+2]环加成反应的产物,然后通过常规化学合成及活性筛选证明该4种产物(syn-TZ2/QA5、syn-6TZ2/QA5、syn-8TZ2/QA5和syn-6TZ2/BA6)具有很强的乙酰胆碱酯酶抑制活性。The solutions of electrophorus AChE with the building blocks were injected directly into the LC/MSD instrument to perform LC/MS-SIM analysis.Then four cycloaddition products were indentified by their retention times and molecular weights.In order to determine the feasibility of the result of in situ click chemistry,the products were synthesized by the conventional click chemistry.The preliminary bioassay showed that all of them exhibited better AChE（electrophorus） inhibitory activity.

关 键 词：液相色谱-质谱 原位点击化学 乙酰胆碱酯酶抑制剂 

分 类 号：O657.7[理学—分析化学]