吡喹酮的分子改性与性能分析-molecular modification and performance analysis of praziquantel.docx

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2018-06-28 发布于上海
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吡喹酮的分子改性与性能分析-molecular modification and performance analysis of praziquantel.docx

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吡喹酮的分子改性与性能分析-molecular modification and performance analysis of praziquantel

MolecularamendingandcharacterizationofpraziquantelAbstractKillingthecercariaelarvaeofschistosomeisanimportantmethodtocutoffthespreadingofschistosomiasis.Sincemorethan98percentofthecercariaelarvaeareusedtofloatingontheair-watersurface,tosucceedinthismethod,weattempttosynthesisamedicinethatcouldself-diffusingalongtheair-waterinterfaceandformamedicinalmembranefloatingonthesurfaceofthewaterimmediately.Inourexperiments,anovelmedicinewasdesignedbasedonthemodificationofpraziquantel.Toendowthemoleculeswiththepropertiesofself-diffusionalongthesurfaceofwaterandfloatingasamembrane,thepolyglycolwascoupledwithpraziquanteltogaintheinterfaceactivities.Inthispaper,thenovelmedicinederivedfrompraziquantelwassynthesizedviaathree-stepreaction.Firstlythepraziquantelwascoupledwithnitrylintheconditionoficebrine.SecondlythenitrylwasdeoxidizedbySnCl2withhydrochloricacid.ThenthecompoundwascoupledwithPEG.Thestructuresofthecompoundswerecharacterizedbytheinfraredmicroscope(IR),magneticresonance(1HNMR)andmassspectrum(MS).Bythemethods,8compoundsweresynthesized.FurtherexperimentsalsorevealedthatthederivativeskepthighkillrateforthecercariaelarvaeofSchistosomejaponicum.ThecompoundsweresolvedbyHCCl3tothedensityof0.5mg/μL.Thesolutionswererejectedtothewaterwhich25~100cercariaelarvaewereplacedinitbyamicro-rejecter.Theconcentrationofthemedicinewas0.13mg/cm2,whilethecercariaelarvaecontactedwiththecompoundofcomp4a、comp4bfor30min,thekillratereachedupto100percent.Asrevealedbythebrewsteranglemicroscope(BAM),whilethemedicinewasdroppedonthesurfaceofthewater,theliquordiffusedalongtheair-waterinterfaceimmediately.Thestateofthemedicineonthesurfaceofthewaterwasalsocharacterizedbytheatomforcemicroscope(AFM).Thedetectedthicknessofthefilmisabout1.0nm,whichindicatedthatthemoleculesarelyingonthesurfaceofthewateruniformly.Keywords:cercariaelarvaeofSchistosome;Praziquantel;self-diffusion;killrate;Brewsteranglemicroscope目录摘要....................................................................................................