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

Abstract: 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, ¹³C 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 64 μg/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 IC₅₀ values ranging from 0.46 μM to 0.86 μM.These compounds demonstrated poor (BuChE) inhibito〖JP3〗ry activity with IC₅₀>100 μM 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.

Key words: synthesis, jatrorrhizine, jatrorrhizine triazoles, antimicrobial activity, acetylcholinesterase (AChE) inhitibitor