糖基噻唑烷-4-酮衍生物的合成及活性評價.pdf

1、河北大學(xué)碩士學(xué)位論文糖基噻唑烷4酮衍生物的合成及活性評價姓名：焦玲玲申請學(xué)位級別：碩士專業(yè)：應(yīng)用化學(xué)指導(dǎo)教師：李小六；陳華200905AbstractsAbstractsThiazolidinoneisofconsiderableimportanceasapharmacophoricgroupduetotheirpotentialbiologicalactivitiessuch舔anti—virus，anti—tumor，bacteri

2、cidal，antiinflammatoryetcTothebestofourknowledge，mostofsuchcompoundsthathavebeenreportedconcentratedonthelipophilicgroupsasthesubstituents，onlyafewreportsonthesynthesisandpharmacologyofthethiazolidinonescontaininghydroph

3、ilicgroupssuchasaminoacid，sugarmoietyhavebeenpublishedtakingintoaccountthecarbohydrateplayanimportantroleontheidentificationofbiologicalmacromoleculessuchasprotein，Inordertoimprovehydrophilicityofmoleculesandenhanceaffin

4、ityofcellsandproteinInthispaperwefocusedonthiazolidine4一onewithlinkedglycosylationasanucleosideanalogueHopetogetsomeleadcompoundswithgoodbiologicalactivityinantivirus，anti—tumorfordrugdevelopment1、Synthesisandbiologicala

5、ctivityofnovelthiazolidin4oneswithacarbohydratemoietySomenovel2aryl3【5deoxy一1，2OisopropylideneaD—xylofuranose一5一C—yl】thiazolidin4onesweresynthesizedbythethreecomponentcondensationof5一amino一5deoxy1，2O—isopropylidenea—Dxyl

6、ofuranose41，aromaticaldehyde，andmercaptoaceticacidinthepresenceofDCCandDMAPatroomtemperatureTwodiastereoisomers44and45wereaffordedasthemainproductsintotallyisolatedyieldsof25470％Thestructuresofthenewcompoundsweredetermin

7、edbyNMRspectroscopyandmassspectrometry(MS)，andtheconfigurationinthiazolidin一4一oneringWastentativelyassignedbasedontheX—raycrystallographicstructureof54dandthecomparisonoftheircorrespondingNMRsignalsTheantitumor(humancerv

8、icalcancercells)activityandtheinhibitionagainsttheglycosidases(口glucosidase，13glucosidase，口amylase)havebeenevaluatedforthenewcompounds，someofwhichexhibitedantitumoractivity2、Synthesisandbiologicalactivityofnovelthiazolid

9、in4oneswithdisaccharidemoietyuseofStaudinger／Aza—WittigreactionDerivativesofazido—glucopyranoseandfuraldehydeweresynthesizeduseofGlucoseandriboseasrawmaterial，synthesisofnovel4thiazolidinonelinkeddisaccharidesbytandemSta

10、udinger／azaWittig／cyclizationinthepresenceofnitrine，aldehyde，andmercaptoaceticacidatroomtemperatureThemainproductsintotallyisolatedyieldsof60％ThedeprotectionofacetylwasontheconditionofsodiummethoxideDiscussiontheinfluenc