新型原卟啉原氧化酶抑制劑的設(shè)計(jì)、合成與生物活性研究.pdf

1、南開(kāi)大學(xué)博士學(xué)位論文新型原卟啉原氧化酶抑制劑的設(shè)計(jì)、合成與生物活性研究姓名：李華斌申請(qǐng)學(xué)位級(jí)別：博士專(zhuān)業(yè)：農(nóng)藥學(xué)指導(dǎo)教師：楊華錚20081001AbstractAbstractsProtoporphyrinogenoxidase(PPO，EC1334)isthelastenzymeinthecommontetrapyrrolebiosynthesispathwaybeforethepathwaybranchestowardchlorop

2、hyllandheinesynthesisPPOinhibitorshavebecomeoneofthemostpopularherbicidesinrecentyearsIncontrasttootherherbicides，PPOinhibitorshavesomegeneralcharacteristics：controlweedsatalowuserate；actrapidly；donotaccumulateinenvironm

3、entanddonotharmmammalsundernormalconditionsForthesecharacteristics，PPOinhibitorsconstituteakindofimportantherbicideTosearchfornewPPOinhibitors，accordingtobiorationaldesignmorethan90novel3Hpyrazolo[3，4d】[1，2，3]triazin4one

4、derivativesweredesignedandsynthesizedAllcompoundshavebeencharacterizedbyelementalanalysesand1HNMRSomeofthemhavebeenfurtherconfirmedby2D—NMR(HSQCandHMBC)andXraysinglecrystaldiffractionAppropriateprotectivegroupswereutiliz

5、edforprotectionofphenolandnitrogenatominpyrazoleringTheprotectivegroupswereremovedwhencompoundsTA一5andTC1wereobtainedAndthenaseriesoftargetcompoundswerederivedfromthemThisallowedtherapidandparallelsynthesisofaseriesofder

6、ivativesThereareseveralassayproceduresforthestudyofinhibitoryactivitiesofPPOinhibitorsTheassayproceduresareutilizedtoevaluatetheeffectsofPPOinhibitorsonPPOactivityprotoporphyrinIXaccumulationandphytotoxicactivityusingsom

7、ehigherplantsAmongthem，assayofPPOinhibitionisutilizedmorefrequentlyforQSARstudyThepls0againstPPOoftargetcompoundswerecarriedoutaccordingtotheprocedurewithmodificationsAndtheherbicidalactivitiesofthecompoundsweretestedThe

8、structureactivityrelationshipofthetargetcompoundswasstudiedaccordingtothebioassaydataMostofthemexhibitedgoodPPOinhibitoryactivitySomeofthemshowedpromisingherbicidalactivityinthegreenhouseTC一14showedexcellentherbicidalact