2022
Accelerating Metabolite Identification Mass Spectrometry Technology Drives Metabolite Identification Studies Forward
NASSAR A. Accelerating Metabolite Identification Mass Spectrometry Technology Drives Metabolite Identification Studies Forward. 2022, 267-302. DOI: 10.1002/9781119851042.ch8.Peer-Reviewed Original ResearchDrug candidatesDrug discoveryLC-MSLiquid chromatography-mass spectrometryChromatography-mass spectrometryMetabolite identification studiesSuccessful drug candidatesFlight mass spectrometryDrug discovery effortsMass spectrometry technologyTriple quadrupoleADMET studiesStructural assignmentMass spectrometryMetabolite characterizationLead compoundsSpectrometry technologyIon trapDiscovery effortsOverall safety profileHuman-specific metabolitesSpectrometryDrug development processMetabolism issuesMetabolite profilingRole of Structural Modifications of Drug Candidates to Enhance Metabolic Stability
Nassar A. Role of Structural Modifications of Drug Candidates to Enhance Metabolic Stability. 2022, 303-322. DOI: 10.1002/9781119851042.ch9.Peer-Reviewed Original ResearchDrug candidatesStructural modificationsMetabolic stabilityDrug discovery processADME propertiesMetabolite characterizationDrug designDrug discoveryBalance of propertiesToxicity relationshipsExcretion studiesMetabolic instabilityDiscovery processHuman patientsStabilityPropertiesSuccess rateModificationDrugsCandidatesCharacterizationAbsorptionPatients
2008
Structural Modifications of Drug Candidates: How Useful Are They in Improving Metabolic Stability of New Drugs? Part I: Enhancing Metabolic Stability
Nassar A. Structural Modifications of Drug Candidates: How Useful Are They in Improving Metabolic Stability of New Drugs? Part I: Enhancing Metabolic Stability. 2008, 253-268. DOI: 10.1002/9780470439265.ch10.Peer-Reviewed Original Research
2006
The impact of recent innovations in the use of liquid chromatography-mass spectrometry in support of drug metabolism studies: are we all the way there yet?
Nassar A, Talaat R, Kamel A. The impact of recent innovations in the use of liquid chromatography-mass spectrometry in support of drug metabolism studies: are we all the way there yet? Current Opinion In Drug Discovery & Development 2006, 9: 61-74. PMID: 16445118.Peer-Reviewed Original ResearchConceptsLC-MSDrug metabolism studiesOptimal balance of propertiesTime-of-flight mass spectrometryCombination of LC-MSDrug discoveryArea of drug metabolismLiquid chromatography-mass spectrometryTriple quadrupoleChiral separationADMET studiesChromatography-mass spectrometryIon trapMetabolite characterizationDrug discovery effortsBalance of propertiesMass spectrometryLead compoundsIsotope labelingMetabolic studiesStable isotope labelingADMETDrug candidatesDiscovery effortsSpectrometry
2004
Improving the decision-making process in the structural modification of drug candidates: enhancing metabolic stability
Nassar A, Kamel A, Clarimont C. Improving the decision-making process in the structural modification of drug candidates: enhancing metabolic stability. Drug Discovery Today 2004, 9: 1020-1028. PMID: 15574318, DOI: 10.1016/s1359-6446(04)03280-5.Peer-Reviewed Original ResearchConceptsStructural modification of drug candidatesDrug candidatesDesign of drug candidatesStructural modificationsDrug discovery processADME propertiesADME studiesMetabolite characterizationBalance of propertiesDecision-making processDrug designMetabolic stabilityDrug discoveryDiscovery processADMEMetabolic instabilityDesignDevelopment stagePropertiesStrategies for dealing with metabolite elucidation in drug discovery and development
Nassar A, Talaat R. Strategies for dealing with metabolite elucidation in drug discovery and development. Drug Discovery Today 2004, 9: 317-327. PMID: 15037231, DOI: 10.1016/s1359-6446(03)03018-6.Peer-Reviewed Original ResearchConceptsMetabolite structural informationDrug discoveryStructural informationMetabolite elucidationMetabolite characterizationDrug candidatesMetabolitesElucidation
2003
Metabolite characterization in drug discovery utilizing robotic liquid-handling, quadruple time-of-flight mass spectrometry and in-silico prediction.
Nassar A, Adams P. Metabolite characterization in drug discovery utilizing robotic liquid-handling, quadruple time-of-flight mass spectrometry and in-silico prediction. Current Drug Metabolism 2003, 4: 259-71. PMID: 12871044, DOI: 10.2174/1389200033489406.Peer-Reviewed Original ResearchConceptsQuadrupole time-of-flight mass spectrometerIdentification of metabolitesChemical structureMetaboLynx softwarePotential metabolitesQuadruple time-of-flight mass spectrometryTime-of-flight mass spectrometerEarly stages of drug discoveryInternal mass calibrationTime-of-flight mass spectrometryIn vitro microsomal incubationsSample preparationStages of drug discoveryReplicate sample injectionsDrug discoveryRobotic liquid handlerHypothetical chemical structureSynthetic chemistsMS/MS spectraMass spectraMetabolite characterizationGradient elutionMass spectrometerHuman hepatic microsomesMicrosomal incubations
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