1，2，3-噻二唑衍生物的分子設(shè)計、合成及生物活性研究.pdf

1、曲阜師范大學(xué)碩士學(xué)位論文1，2，3噻二唑衍生物的分子設(shè)計、合成及生物活性研究姓名：楊知昆申請學(xué)位級別：碩士專業(yè)：化學(xué)有機化學(xué)指導(dǎo)教師：尤進(jìn)茂范志金20090401AbstractAbstractForty—ninenoveldiheterocycliccompoundscontainingboth12，3thiadiazoleand12，4triazolemoietiesweredesignedandsynthesizedaccordi

2、ngtotheprinciplesofcombinationofbioactivesub—structuresOilthebasisofsystemicconclusionofthestudyprogressonI，23thiadiazolederivativesandl，24triazolederivativesinthisthesisA1lthestructuresofthetargetcompoundssynthesizedwer

3、edeterminedby1HNMRandIRsomeofthemweredeterminedbyelementalanalysisandEl—MS，twotypicalcrystalsofI7andII3wereculturedanddetectedforstructureconfirmationbyX—raycrystaldiffractionThetitlecompoundsCanbedividedintotwoseriesacc

4、ordingtotheirstructuralcharacteristicsas6substituted3一(4一methyl一12，3一thiadiazolyl)一[1，2，4]triazolo一【3，4一們【l，3，4]thiadizoles(I)and4一substitutedimino一3一(4一methyl一1，2，3thiadiazolyl)一1，2，4一triazole一5一thione(n)，theirstructure

5、swereshownasfollowing：N“NNJINIISRPreliminarybiologicalactivityscreeningindicatedthat，allthecompoundsshowedcertaindegreesoffungicidalactivityagainstmostfungitestedat501xg／mLThegrowthinhibitionrateofcompounds124，125，h6，136

6、，113，Ih，116and1112againstBotrytiscinereawereupto80％122exhibitedgoodgrowthinhibitiontomosttestedfungiwiththegrowthinhibitionrateagainstPhysalosporapiricola，PelliculariasasakiimoreandRhizoctoniasolaniwereallupto83％，theECs0

7、against6fungiwerebetween25Itg／mLand146tg／mL，thiscompoundCanbeconductedforfurtherstudiesausfungicideleadingcompoundWhile，125exhibitedgoodfungicideactivityagainstFusariumoxysporumwithgrowthinhibitionrateof93O％CompoundsIIex

8、hibitedgoodfungicideactivityagainstBotrytiscinema，thegrowthinhibitionofcompoundIIz2wasupto87％，compounds113，114and116hadabout78％ofgrowthinhibitionandcompound111hadgoodactivityagainstGibberellazeae、析thgrowthinhibitionof787

9、％InvitroinhibitionrateofcompoundIllagainstTMVWaS5357％at500pg／mL，whichWasbetterthanthatofpositivecontroleribavirindidCompound17hadgoodantivirusactivityagainstTMVwinlinhibitionrateof4444％bothat100Itg／mLand500rtg／mLMosttarg