雜環(huán)不對稱芳香二硫醚類化合物的分子設(shè)計、合成及其活性研究.pdf

1、南開大學(xué)碩士學(xué)位論文雜環(huán)不對稱芳香二硫醚類化合物的分子設(shè)計、合成及其活性研究姓名：王偉民申請學(xué)位級別：碩士專業(yè)：農(nóng)藥學(xué)指導(dǎo)教師：王建國201205AbstractAbstractInbacterium，epiphyte，seaweedsandplants，AHAS(Acetohydroxyacidsynthase)isthekeyenzymeinvolvedintheprocessofbiosynthesisthebranchedcha

2、inaminoacidsbutinanimalsitisn’tfoundSo，AHASinhibitorsareoneofthemostactiveareasoftheherbicidedevelopmentAHASinhibitorspeciesintheglobalherbicidemarketaremainlythefollowingfourcategories：sulfonylurea，imidazolinone，pyrimid

3、inesalicylicacid，andsulfonamidesBasedontheAHASthree—dimensionalcrystalstructure，wefilteroutsomeofthenewstructureofAHASinhibitorsbythemeansofvirtualscreeningAccordingtotheCharacteristicsofthehiredmolecularstructure，Combin

4、edwithpreviousstudiesofourgroup，wetearoffandthemodeofexistingtypicalstructureofAHASinhibitors，designandsynthesisofheterocyclicasymmetricaromaticdisulfidecompoundsThesecompoundshavebeencharacterizedby1HNMR，IR，MSandFTMS111

5、estructureofI3hasbeenfurtherconfirmedbyXraycrystaldiffractionanalysis而esynthesizedcompoundswerecarriedoutinvitroandinvivobioassayandthetestresultsindicatethatthesecompoundsshowsomeinhibitoryactivityAmongthem，Inhibitoryra

6、tesofcompoundI5andI6towildtypeAtAHASaregreaterthan95％intheconcentrationof1001xg／mL，theresultsofsmallglasspetridishat1001xg／mLare926％and878％Inhibitionrateofamaranthinthepotexperiment，themeasuredtwocompoundsat100g／acreareb

7、oth100％WealsodotheexogenousbranchedchainaminoacidrecoveryexperimentsComparetheblankcontrolswithbranchedchainaminoacidtothosewithoutbranchedchainaminoacid，wefindevenbranchedchainaminoacidsalsoinhibitthegrowthofraperootWim

8、compoundsI5，theraperootlengthinhibitionissignificantlylowerthanthatwithbranchedchainaminoacidsTheresultsshowtheactivityofheterocyclicasymmetricaromaticdisulfidecompoundsrelateswiththebiosynthesisofbranchedchainaminoacidb