摘要
通过有机合成手段合成了四个新的含三唑的药根碱衍生物,利用1H NMR,13C NMR和MS确认了目标化合物的结构,对合成的化合物进行了抗菌和抑制乙酰胆碱酯酶(ACh E)和丁酰胆碱酯酶(Bu Ch E)的活性测试。目标化合物显示具有较好的抗菌活性,抗菌结果显示所制备的化合物抑菌MIC范围从1到64μg/m L,对一些敏感菌的活性和阳性药物罗红霉素相当。对乙酰胆碱酯酶(ACh E)的抑制也表现出较好的活性,IC50值从0.46μM到0.86μM,但这些化合物对丁酰胆碱酯酶(Bu Ch E)表现出较弱的活性IC50>100μM。药根碱三唑具有较好的抑制乙酰胆碱酯酶的活性,且具有较好的选择性,同时具有较好的抗菌活性而且拓展了抗菌谱,可能成为一种新型的抗菌和治疗老年痴呆的先导化合物。
Four new jatrorrhizine triazoles were designed and synthesized by means of organic synthesis with expectation of increasing the antimicrobial activity and inhibitory activity on acetylcholinesterase,their structures were characterized by 1H NMR,13 C NMR,and MS spectra data.All target compounds were evaluated for antimicrobial activities in vitro and their biological activities as inhibitors of both acetylcholinesterase(AChE)and butyrylcholinesterase(BuChE)were evaluated.The results of antimicrobial activities indicated that the prepared compounds exhibited potent antibacterial with low MIC values ranging from 1 to 64μg/mL,which were comparable to or even better than those of the reference drug Roxithromycin.Additionally,All target compounds were found to be potent inhibitor of AChE,with low IC 50 values ranging from 0.46μM to 0.86μM.These compounds demonstrated poor(BuChE)inhibito ry activity with IC 50>100μM for butyrylcholinesterase(BuChE),Jatrorrhizine triazoles exhibited the good activity of inhibiting acetylcholinesterase,in the meantime exhibitied higher selectivity for AChE over BuChE,it is suggested that Jatrorrhizine triazoles might become agents for Alzheimer’s disease(AD).at the same time Jatrorrhizine triazoles show good antibacterial activity and expand the antibacterial spectrum,Jatrorrhizine triazoles maybe apotential antibacterial agents.
作者
蒋小飞
张伟
熊南茜
JIANG Xiao-fei;ZHANG Wei;XIONG Nan-qian(School of Chemistry and life sciences,Guizhou University of Education 550018,P.R.China;College of Chemical and Environmental Engineering,Chongqing Three Gorges University 404000,P.R.China;School of Geography and Tourism,Guizhou Education University 550018,P.R.China)
出处
《天然产物研究与开发》
CAS
CSCD
北大核心
2018年第4期535-540,共6页
Natural Product Research and Development
基金
国家自然科学基金(41573081)
重庆市教委基金资助项目(KJ131120)
贵州省自然科学基金(3001433)
关键词
合成
药根碱
药根碱三唑
抗菌活性
乙酰胆碱酯酶抑制剂
synthesis
jatrorrhizine
jatrorrhizine triazoles
antimicrobial activity
acetylcholinesterase(AChE)inhitibitor
