药学专业英语视听说教程 课件 视听说上篇Lecture 6 Medicinal Chemistry.pptx

Lecture6MedicinalChemistry

enantiomerprodruglipophilicityalkylatecycloaddition

interdisciplinaryesteramidekinasehydrolytic

drugdesignsmall-moleculedrugschemotherapeuticrefiningdrug-likeagentspreclinical

syntheticorganicchemistrycombinepharmacokineticspharmacodynamics

1.Threewaystoimprovethetherapeuticefficacyofadrug:1)Thebiologicalapproachto__________________________________________;2)Thephysicalapproachto____________________________________________;3)Thechemicalapproachto___________________________________________.2.Theidealpropertiesofaprodrug:1)Drugandthecarrierlinkagemustbe___________________________________;2)Itshouldnothave_________________________________________________;3)Itshouldrapidly___________________________________________________;4)Themetabolicfragmentsshouldbe____________________________________.altertherouteofadministrationmodifythedesignofthedosageformenhancedrugselectivityandminimizetoxicityclearedinvivointrinsicpharmacologicalactivitytransformintotheactiveformnon-toxic

3.Characteristicsofthecarrierlinkedprodrugs:?Structure—_________________________________________________________________________________________________________?Chemicalnature—________________________________________?Mechanismofreleasingtheactivedrug—______________________ortransportmoietytheactivedrugbeingcovalentlylinkedtoaninertcarrierestersoramideswithgreatlymodifiedlipophilicityhydrolyticcleavage

()1.Manydrugsarechiralmoleculeswithatleastonechiralitycenter,existinginenantiomerswhicharemirrorimagestoeachother.()2.Itispossibletosynthesizeonlyoneenantiomerofachiraldrugwithoutsynthesizingtheotherenantiomeratthesametime.()3.Itisverycommonthatbothenantiomersofachiraldrugarebiologicallyactiveandhavedesirableeffectonourbody.()4.Onlyoneoftheenantiomersofthalidomidewasusefulint