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OrganomedicinalChemistryThePurposeofCourseTheContentsofCourseCourseEvaluationMethodGeneralaspectsofmedicinalchemistryDefinition,conceptsandobjectivesWhat’sMedicinalChemistry?WhatMedicinalChemistryMainStepsinFindingADrugWhatADrugIsDoingIntheBody?WhatAretheThreePhasesGoverningADrugActivity?HowDoesMetabolismAffectDrugActivity?DrugEliminationinDifferentRateDrugClassificationsandNamesMeasurementandExpressionofDrugEffectsMechanismofDrugEffectsMeasurementofDrugEffectsAgonist,Antagonist,PartialAgonistandInverseAgonistAnalysisofLigand-ReceptorInteractionDoseandEffectsCureorDeath?DrugTargetsandMechanismofActionModeofActionofAgonistsandAntagonistsLeadCompoundDiscoveryStrategy(II)StrategiesinthesearchfornewleadcompoundsororiginalhypothesisFirstStrategy:ImprovementofExistingDrugsFirstStrategy:ImprovementofExistingDrugsSecondStrategy:SystematicScreeningScreeningIntermediatesandOldDrugsThirdStrategy:ExploitationofBiologicalInformationFourStrategy:PlannedResearchandRationalApproachesInhibitorsoftheangiotensin-convertingenzymeInteractionmodellingDiscoverycoursefortheinhibitorsDiscoveryCourseforH2-ReceptorAntagonistsComputer-AideddrugdesignKeyIssuesofLeadDiscoveryMeansNaturalProductsPenicilinCombinatorialChemistry(I)CombinatorialChemistry(II)CombinatorialChemistry(III)DrugorNon-drug?(I)DrugorNon-drug?(II)DrugorNondrug?(III)PrimaryExplorationofStructure-ActivityRelationshipsHomologous,VinyloguesandBenzologuesVariationHomologousmoleculesmethylenegroupdifferencesHomologousSeriesandBiologicalResponseCurvesA.Bell-ShapedCurvesB.ApparentlyContinuousIncreaseCurvesC.ZigzagShapedCurvesVinyloguesandBenzologuesBenzologueExampleIsostericReplacementsWhat’sIsosterismandBioisosterim?InterchangesBetweenMonovalent,BivalentandTrivalentAtomsorGroupsRingEquivalentReplacementsSurrogatesofCarboxylicAcidSurrogatesofEsterSurrogatesofamideandpeptideSurrogatesofPhenolandUreaIsosteresviaPositionalExchangesFluorineReplacementsConformationalRestrictionsandStericHindranceinMedicinalChemistryAnalogueApproaches(I)R