Study On Structural Modifications Of Areca Alkaloids And Antibacterial Activity Of Areca Alkaloids Derivatives In Vitro

Aim:Areca alkaloids,which have a certain antibacterial activity,are the main active ingredients of traditional chinese medicine betel nut.Through modern organic chemical methods the structural modifications of areca alkaloids are achieved.A series of areca alkaloids derivatives are prepared from availableβ-ketoamides andα,β-unsaturated aldehydes.The research about the antimicrobial activity in vitro is carried out in order to screen out the compouds with higher activity and a wider antibacterial range.Methods:1.A series of areca alkaloids derivatives with the cyclopentane and spiro-piperidine units are synthesized by two different catalytic activation mode（HOMO and LUMO）.The structures are derived by HRMS,¹H-NMR,¹³C-NMR,and X-Ray single crystal diffraction;2.The minimal inhibitory concentrations in vitro of the newly designed areca alkaloids derivatives are determined by agar double dilution method.Results:In this thesis,a total of 34 products which have not been reported are prepared.The structures are comfirmed by ¹H-NMR,¹³C-NMR,HRMS and X-Ray single crystal diffraction;2.The research about antibacterial activity in vitro indicates that all target products have a certain antibacterial activity which are better than arecoline.Conclusion:The areca alkaloids derivatives synthesized in this thesis have a certain antibacterial activity.