Metabolism, Pharmacokinetics and Toxicity of Functional Groups: Impact of the Building Blocks of Medicinal Chemistry on ADMETCheck Access
Until now, the area of drug metabolism and pharmacokinetics has been lacking in texts written for the Medicinal Chemist. This outstanding book, aimed at postgraduate medicinal chemists and those working in industry, fills this gap in the literature. Written by medicinal chemists and ADMET scientists with a combined experience of around 300 years, this aid to discovering drugs addresses the absorption, distribution, metabolism, excretion and toxicity (ADMET) issues associated with drugs. The book starts by describing drug targets and their structural motifs before moving on to explain ADMET for the medicinal chemist. It is the functional groups which most profoundly influence the drug molecules of which they form a part. They characterise the pharmacology, are essential to the activity, and alter the ADMET characteristics of each drug. Their effects follow a pattern, thus allowing medicinal chemists to predict and overcome potential challenges. For this reason, the Editors have taken the unique approach of dividing the remainder of the book into chapters which each focus on a different functional group. They describe drugs containing the functional group under consideration, explain why the group is there, and outline its physicochemical properties before going on to detail the ADMET issues. Where possible, prodrugs and bioisosteres, which may give alternative ADMET outcomes, are described. The chapters cross refer where similar matters are covered but individual chapters can be used in a stand alone manner. The book ends with a discussion of future targets and chemistry needs.
Metabolism, Pharmacokinetics and Toxicity of Functional Groups: Impact of the Building Blocks of Medicinal Chemistry on ADMET, The Royal Society of Chemistry, 2010.
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Drugs and their Structural Motifsp1-60ByAlexander A. Alex;Alexander A. AlexPfizer Global Research and DevelopmentRamsgate RoadSandwichKentUKCT13 9NJSearch for other works by this author on:R. Ian StorerR. Ian StorerPfizer Global Research and DevelopmentRamsgate RoadSandwichKentUKCT13 9NJSearch for other works by this author on:
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Chapter 2: ADMET for the Medicinal Chemistp61-98ByK. Beaumont;K. BeaumontDepartment of PharmacokineticsDynamics and MetabolismSearch for other works by this author on:S. M. Cole;S. M. ColeDepartment of PharmacokineticsDynamics and MetabolismSearch for other works by this author on:K. Gibson;K. GibsonDepartment of Medicinal Chemistry, Pfizer Global Research and DevelopmentSandwich LaboratoriesSandwichKentCT13 9NJUKSearch for other works by this author on:J. R. GossetJ. R. GossetDepartment of PharmacokineticsDynamics and MetabolismSearch for other works by this author on:
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Chapter 3: Carboxylic Acids and their Bioisosteresp99-167ByAmit S. Kalgutkar;Amit S. KalgutkarPharmacokinetics, Dynamics and Metabolism DepartmentPfizer Global Research and DevelopmentEastern Point RoadGrotonConnecticut06340USASearch for other works by this author on:J. Scott DanielsJ. Scott DanielsPharmacokinetics, Dynamics and Metabolism DepartmentPfizer Global Research and Development700 Chesterfield Village ParkwayChesterfieldMissouri63107USASearch for other works by this author on:
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Chapter 4: Primary, Secondary and Tertiary Amines and their Isosteresp168-209ByD. K. Walker;D. K. WalkerPharmacokinetics, Dynamics and MetabolismPfizer Global Research and DevelopmentRamsgate RoadSandwichKentCT13 9NJUKSearch for other works by this author on:R. M. Jones;R. M. JonesPharmacokinetics, Dynamics and MetabolismPfizer Global Research and DevelopmentRamsgate RoadSandwichKentCT13 9NJUKSearch for other works by this author on:A. N. R. Nedderman;A. N. R. NeddermanPharmacokinetics, Dynamics and MetabolismPfizer Global Research and DevelopmentRamsgate RoadSandwichKentCT13 9NJUKSearch for other works by this author on:P. A. WrightP. A. WrightPharmacokinetics, Dynamics and MetabolismPfizer Global Research and DevelopmentRamsgate RoadSandwichKentCT13 9NJUKSearch for other works by this author on:
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Chapter 5: Sulfonamide as an Essential Functional Group in Drug Designp210-274ByAmit S. Kalgutkar;Amit S. KalgutkarPharmacokinetics, Dynamics and Metabolism DepartmentPfizer Global Research and DevelopmentEastern Point RoadGrotonConnecticut06340USASearch for other works by this author on:Rhys Jones;Rhys JonesPharmacokinetics, Dynamics and Metabolism DepartmentPfizer Global Research and DevelopmentRamsgate RoadSandwichKentUKCT139NJSearch for other works by this author on:Aarti SawantAarti SawantPharmacokinetics, Dynamics and Metabolism DepartmentPfizer Global Research and DevelopmentEastern Point RoadGrotonConnecticut06340USASearch for other works by this author on:
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Chapter 6: Influence of Aromatic Rings on ADME Properties of Drugsp275-327ByDeepak Dalvie;Deepak DalviePharmacokinetics, Dynamics and Metabolism and Department of Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:Sajiv Nair;Sajiv NairPharmacokinetics, Dynamics and Metabolism and Department of Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:Ping Kang;Ping KangPharmacokinetics, Dynamics and Metabolism and Department of Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:Cho-Ming LoiCho-Ming LoiPharmacokinetics, Dynamics and Metabolism and Department of Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:
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Chapter 7: Influence of Heteroaromatic Rings on ADME Properties of Drugsp328-369ByDeepak Dalvie;Deepak DalvieDepartments of Pharmacokinetics, Dynamics and Metabolism and Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:Ping Kang;Ping KangDepartments of Pharmacokinetics, Dynamics and Metabolism and Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:Cho-Ming Loi;Cho-Ming LoiDepartments of Pharmacokinetics, Dynamics and Metabolism and Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:Lance Goulet;Lance GouletDepartments of Pharmacokinetics, Dynamics and Metabolism and Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:Sajiv NairSajiv NairDepartments of Pharmacokinetics, Dynamics and Metabolism and Medicinal ChemistryPfizer Global Research and DevelopmentSan DiegoCA 92121USASearch for other works by this author on:
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Chapter 8: Peptidomimetics and Peptides as Drugs: Motifs Incorporated to Enhance Drug Characteristicsp370-389ByTracey Boyden;Tracey BoydenDepartment of Pharmacokinetics Dynamics and MetabolismPfizer Global Research and DevelopmentEastern Point RoadGrotonCT 06340USASearch for other works by this author on:Mark Niosi;Mark NiosiDepartment of Pharmacokinetics Dynamics and MetabolismPfizer Global Research and DevelopmentEastern Point RoadGrotonCT 06340USASearch for other works by this author on:Alfin Vaz*Alfin Vaz*Department of Pharmacokinetics Dynamics and MetabolismPfizer Global Research and DevelopmentEastern Point RoadGrotonCT 06340USASearch for other works by this author on:
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Chapter 9: Pharmacokinetics and Metabolism of Compounds that Mimic Enzyme Transition Statesp390-459ByIain Gardner;Iain GardnerPharmacokinetics, Dynamics and MetabolismPfizer Global Research and DevelopmentSandwichKentCT13 9NJUKSearch for other works by this author on:Chris Barber;Chris BarberWorldwide Medicinal ChemistryPfizer Global Research and DevelopmentSandwichKentCT13 9NJUKSearch for other works by this author on:Martin Howard;Martin HowardDrug Metabolism and Pharmacokinetics Discovery ResearchPharmaceuticals Division F. Hoffmann-La Roche LTDCH-4070 BaselSwitzerlandSearch for other works by this author on:Aarti Sawant;Aarti SawantPharmacokinetics, Dynamics and MetabolismPfizer Global Research and DevelopmentEastern Point RoadGrotonCT 06340USASearch for other works by this author on:Kenny WatsonKenny WatsonPharmacokinetics, Dynamics and MetabolismPfizer Global Research and DevelopmentSandwichKentCT13 9NJUKSearch for other works by this author on:
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Chapter 10: Alcohols and Phenols: Absorption, Distribution, Metabolism and Excretionp460-485ByZhuang Miao;Zhuang MiaoPfizer Research and DevelopmentGroton LaboratoriesCTUSASearch for other works by this author on:R. Scott ObachR. Scott ObachPfizer Research and DevelopmentGroton LaboratoriesCTUSASearch for other works by this author on:
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Chapter 11: Future Targets and Chemistry and ADME Needsp486-511ByDennis A. Smith;Dennis A. SmithPharmacokinetics, Dynamics and Metabolism and Medicinal ChemistryPfizer Global R & D, SandwichKentCT13 9NJUKSearch for other works by this author on:David S. MillanDavid S. MillanPharmacokinetics, Dynamics and Metabolism and Medicinal ChemistryPfizer Global R & D, SandwichKentCT13 9NJUKSearch for other works by this author on:
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