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1、KJM5230-Biologiskaktivemolekyler(BioactiveMolecules)Thecourcediscusstheorganicchemistryofimportantclassesofdrugsandbioactivenaturalproducts.Synthesis/biosynthesis,modeofaction,bioavailabilityandstabilityforchosendrugclasses.StructureactivityandstructureoptimalisationKJM5230-H06Natur
2、alProductsDrugDesignReseptors-DrugActionDrugMetabolismAntibiotics/AntimicrobialAgentsAntiparasiticAgentsAntifungalAgentsAntimycobacterialAgentsAnticancerAgentsAntiviralAgentsKJM5230-H06OriginofDrugs/BioactiveCompoundsNaturalProducts/NaturalProductDerivativesRandomtesting,serendipity
3、*ScreeningofLibraries(Rational)DrugDesign(1.mentionedSciFinder1970,mostpapersafter1990)Screening/Design/SerendipityLeadcompound-Design/StructureOptimisationActualDrugWhynewdrugs?ResistanceNewdiseases(Aging,lifestyle)LesstolleranceforsideeffectsActivityToxicityBioavailabilityMetaboli
4、sminvitroinvivoanimalsinvivohumans*Fortunatediscoverybyaccident“ThethreeprincesofSerendip”PersianFairytailSerendip=SriLankaKJM5230-H06OriginofDrugs/BioactiveCompounds:HistoryBefore1800:Plants,plantextracts,inorganicmaterial1805:Morphineisolatedfromopium(sructureproposed1935,proovedb
5、ysynth.1952)1828:Firstorganicsynthesis(urea)1840-1850:Firstsynthesizedorg.compdsusedinmedicine:CHCl3,Et2Oanestechia)Exofearlysyntheticdrugs:Choralhydrate(sleepingpill)1869Acetylsalicylicacidsynth1853,clintrials1893Phenazonesynth1884Benzocaine1902Prontocil1932Exofearlyisolatednat.pro
6、d.Quinineca1825Digitoxin1841(structure1928)Salicylicacid,antipyretic1875Cocaineisol.1860,localanestethic1884Benzylpenicillin1941TraditionalmedicineScreeningSerendipityKJM5230-H06NaturalProductsOnlysourceofdrugsbeforelastpartof19thcenturyAntibiotics1940-1960Cyclosporin(immunomodulato
7、r)isolatedfromsoilfungusHardangervidda1971Taxolisolated1960s,approveddrugUSA1992LeadcompoundsKJM5230-H06NaturalProductsSourcesMicroorganisms(bacteria,fungus)-AntibioticsHigherplants,ex.morphine,quinine,taxolSponges(polycellular“animals”,norealorgansorcelltissue)ex.agelasinesHigheran
8、imals,fewerexamples
