Drug discovery today |
Pubbl/distr/stampa | [Kidlington, Oxford], : Elsevier Science Ltd |
Soggetto topico |
Drugs - Design
Pharmaceutical technology Drug Design Technology, Pharmaceutical Médicaments - Conception Techniques pharmaceutiques |
Soggetto genere / forma |
Periodical
periodicals. Periodicals. Périodiques. |
Soggetto non controllato | Pharmacy, Therapeutics, & Pharmacology |
ISSN | 1878-5832 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Periodico |
Lingua di pubblicazione | eng |
Altri titoli varianti | DDT |
Record Nr. | UNINA-9910145568503321 |
[Kidlington, Oxford], : Elsevier Science Ltd | ||
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Lo trovi qui: Univ. Federico II | ||
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Drug formulation design / / Rahul Shukla, Aleksey Kuznetsov, Akbar ʿAlī, editors |
Pubbl/distr/stampa | London : , : IntechOpen, , 2023 |
Descrizione fisica | 1 online resource (328 pages) |
Disciplina | 615.19 |
Soggetto topico | Drugs - Design |
ISBN | 1-83768-472-3 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto | 1. Preformulation Studies: A Versatile Tool in Formulation Design By Kailash Ahirwar and Rahul Shukla 2. Formulation by Design: An Overview By Ushasi Das, Dilip Kumar Panda and Sanchita Mandal 3. Metal-Based Nanomaterials Photodynamic Action with a Focus on Au and Ag Nanomaterials By Atiyeh Nomani, Anvarsadat Kianmehr, Shahriyar Abdoli and Siamak Javani 4. Development of Liquisolid Compacts: An Approach for Dissolution Enhancement of Poorly Aqueous Soluble Drugs By Madhavi Kasturi 5. Lipid as a Vehicle/Carrier for Oral Drug Delivery By Jagruti Desai, Tapan Desai and Ashwini Patel 6. Xylan-Based Hydrogels: A Polymeric Carrier for Sustained and Targeted Delivery of Drugs By Samit Kumar, Amit Kumar and Dinesh K. Mishra 7. Porphyrinoid Photosensitizers for Targeted and Precise Photodynamic Therapy: Progress in Fabrication By Devika Sivakumar, Rakhi Raju, Y.T. Kamal, Shahana Salam, Sabna Kotta and Rahul Soman 8. Synthesis of Glycoconjugates in Potentiating Pharmacological and Pharmaceutical Activity By Smita Kumbhar and Manish Bhatia 9. A Scientific Ethnomedical Study Using Microbes on Gaucher Disease: An In-Silico Analysis By Sreeram Sudhir and Amritha Pozhaiparambil Sasikumar 10. Spectrophotometric/Titrimetric Drug Analysis By Nagib Qarah and Ezzouhra El-Maaiden 11. Chemistry and Modern Techniques of Characterization of Co-Crystals By Akbar Ali, Aleksey Kuznetsov, Muhammad Ibrahim, Azhar Abbas, Nadia Akram, Tahir Maqbool and Ushna 12. Modification of Physicochemical Properties of Active Pharmaceutical Ingredient by Pharmaceutical Co-Crystals By Raju Thenge, Vaibhav Adhao, Gautam Mehetre, Nishant Chopade, Pavan Chinchole, Ritesh Popat, Rahul Darakhe, Prashant Deshmukh, Nikesh Tekade, Bhaskar Mohite, Nandu Kayande, Nilesh Mahajan and Rakesh Patel 13. Co-Crystallization Techniques for Improving Nutraceutical Absorption and Bioavailability By Asmita Gajbhiye, Debashree Das and Shailendra Patil 14. Co-Crystallization of Plant-Derived Antimalarial Drugs: An Alternate Technique for Improved Physicochemical Qualities and Antimalarial Drug Synergy By Zakio Makuvara. |
Record Nr. | UNINA-9910727276803321 |
London : , : IntechOpen, , 2023 | ||
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Lo trovi qui: Univ. Federico II | ||
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Drug invention today |
Pubbl/distr/stampa | [Madhya Pradesh, India], : [Drug Invention Today], [2009]- |
Soggetto topico |
Drug development
Drugs - Design Pharmacology Drug Design Drug Discovery Pharmaceutical Preparations Pharmacy |
Soggetto genere / forma |
Periodical
Fulltext Internet Resources. Periodicals. |
ISSN | 0975-7619 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Periodico |
Lingua di pubblicazione | eng |
Altri titoli varianti | DIT |
Record Nr. | UNINA-9910140041503321 |
[Madhya Pradesh, India], : [Drug Invention Today], [2009]- | ||
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Lo trovi qui: Univ. Federico II | ||
|
Drug invention today |
Pubbl/distr/stampa | [Madhya Pradesh, India], : [Drug Invention Today], [2009]- |
Soggetto topico |
Drug development
Drugs - Design Pharmacology Drug Design Drug Discovery Pharmaceutical Preparations Pharmacy |
Soggetto genere / forma |
Periodical
Fulltext Internet Resources. Periodicals. |
ISSN | 0975-7619 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Periodico |
Lingua di pubblicazione | eng |
Altri titoli varianti | DIT |
Record Nr. | UNISA-996210289103316 |
[Madhya Pradesh, India], : [Drug Invention Today], [2009]- | ||
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Lo trovi qui: Univ. di Salerno | ||
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Drug metabolism in drug design and development [[electronic resource] ] : basic concepts and practice / / edited by Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys |
Pubbl/distr/stampa | Hoboken, N.J., : Wiley-Interscience, c2008 |
Descrizione fisica | 1 online resource (633 p.) |
Disciplina |
615.7
615/.7 |
Altri autori (Persone) |
ZhangDonglu
ZhuMingshe HumphreysW. Griffith |
Soggetto topico |
Drugs - Metabolism
Drugs - Design Drug development |
ISBN |
1-281-09423-4
9786611094232 0-470-19169-4 0-470-19168-6 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
DRUG METABOLISM IN DRUG DESIGN AND DEVELOPMENT; CONTENTS; Preface; Contributors; PART I BASIC CONCEPTS OF DRUG METABOLISM; 1 Overview: Drug Metabolism in the Modern Pharmaceutical Industry; 1.1 Introduction; 1.2 Technology; 1.3 Breadth of Science; 1.3.1 Chemistry; 1.3.2 Enzymology and Molecular Biology; 1.4 Impact of Drug Metabolism on Efficacy and Safety; 1.4.1 Efficacy; 1.4.2 Safety; 1.5 Regulatory Impact and IP Position; 1.6 Summary; References; 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs; 2.1 Introduction; 2.2 Nomenclature and Terminology
2.3 General Features of the Enzymes2.4 Fractional Contributions of Different Enzymes; 2.5 Oxidation Enzymes; 2.5.1 Cytochrome P450 (P450, CYP); 2.5.2 Flavin-Containing Monooxygenase (FMO); 2.5.3 Monoamine Oxidase (MAO); 2.5.4 Aldehyde Oxidase and Xanthine Dehydrogenase; 2.5.5 Peroxidases; 2.5.6 Alcohol Dehydrogenases (ADH); 2.5.7 Aldehyde Dehydrogenases (ALDH); 2.6 Reduction; 2.6.1 P450, ADH; 2.6.2 NADPH-P450 Reductase; 2.6.3 Aldo-Keto Reductases (AKR); 2.6.4 Quinone Reductase (NQO); 2.6.5 Glutathione Peroxidase (GPX); 2.7 Hydrolysis; 2.7.1 Epoxide Hydrolase; 2.7.2 Esterases and Amidases 2.8 SummaryReferences; 3 Conjugative Metabolism of Drugs; 3.1 UDP-Glucuronosyltransferases; 3.1.1 Location Within the Cell; 3.1.2 Endogenous Substrates; 3.1.3 Enzyme Multiplicity; 3.1.4 Inducibility; 3.1.5 Pharmacogenetics; 3.1.6 Experimental Considerations; 3.1.7 Enzyme Selective Substrates and Inhibitors; 3.1.8 Drug-Drug Interactions and Glucuronidation; 3.1.9 Summary; 3.2 Cytosolic Sulfotransferases; 3.2.1 Cellular Location and Tissue Expression; 3.2.2 The SULT Superfamily of Cytosolic Enzymes; 3.2.3 Inducibility; 3.2.4 SULT Pharmacogenetics 3.2.5 Analytical Detection of Sulfonated Metabolites3.2.6 SULT Inhibitors (Pacifici and Coughtrie, 2005); 3.2.7 Drug-Drug Interactions and Sulfonation; 3.2.8 Summary; 3.3 Glutathione-S-Transferases; 3.3.1 General Overview; 3.3.2 Classification of the GST Enzymes; 3.3.3 Localization and Expression; 3.3.4 Reactions Catalyzed by GSTs; 3.3.5 Regulation of GSTs; 3.3.6 GST Alpha Class; 3.3.7 GST Mu Class; 3.3.8 GST Pi Class; 3.3.9 GST Theta Class; 3.3.10 GST Zeta Class; 3.3.11 Incubation Conditions and Analytical Methods; 3.3.12 Glutathione Conjugate Metabolism (Mercapturic Acid Pathway) References4 Enzyme Kinetics; 4.1 Introduction; 4.2 Enzyme Catalysis; 4.3 Michaelis-Menten Kinetics; 4.3.1 Meanings of K(m), V(max) and Their Clinical Relevance; 4.4 Graphical Kinetic Plots; 4.5 Atypical Kinetics-Allosteric Effects; 4.5.1 Overview of Atypical Kinetic Phenomena; 4.5.2 Homotropic Cooperativity; 4.5.3 Heterotropic Cooperativity; 4.6 Graphical Analysis of Atypical Kinetic Data; 4.7 Enzyme Inhibition Kinetics; 4.7.1 Overview; 4.7.2 Competitive Inhibition; 4.7.3 Mixed Inhibition; 4.7.4 Noncompetitive Inhibition; 4.7.5 Uncompetitive Inhibition 4.7.6 Summary of Effects of Various Inhibition Types of Kinetic Parameters |
Record Nr. | UNINA-9910143981703321 |
Hoboken, N.J., : Wiley-Interscience, c2008 | ||
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Lo trovi qui: Univ. Federico II | ||
|
Drug metabolism in drug design and development [[electronic resource] ] : basic concepts and practice / / edited by Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys |
Pubbl/distr/stampa | Hoboken, N.J., : Wiley-Interscience, c2008 |
Descrizione fisica | 1 online resource (633 p.) |
Disciplina |
615.7
615/.7 |
Altri autori (Persone) |
ZhangDonglu
ZhuMingshe HumphreysW. Griffith |
Soggetto topico |
Drugs - Metabolism
Drugs - Design Drug development |
ISBN |
1-281-09423-4
9786611094232 0-470-19169-4 0-470-19168-6 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
DRUG METABOLISM IN DRUG DESIGN AND DEVELOPMENT; CONTENTS; Preface; Contributors; PART I BASIC CONCEPTS OF DRUG METABOLISM; 1 Overview: Drug Metabolism in the Modern Pharmaceutical Industry; 1.1 Introduction; 1.2 Technology; 1.3 Breadth of Science; 1.3.1 Chemistry; 1.3.2 Enzymology and Molecular Biology; 1.4 Impact of Drug Metabolism on Efficacy and Safety; 1.4.1 Efficacy; 1.4.2 Safety; 1.5 Regulatory Impact and IP Position; 1.6 Summary; References; 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs; 2.1 Introduction; 2.2 Nomenclature and Terminology
2.3 General Features of the Enzymes2.4 Fractional Contributions of Different Enzymes; 2.5 Oxidation Enzymes; 2.5.1 Cytochrome P450 (P450, CYP); 2.5.2 Flavin-Containing Monooxygenase (FMO); 2.5.3 Monoamine Oxidase (MAO); 2.5.4 Aldehyde Oxidase and Xanthine Dehydrogenase; 2.5.5 Peroxidases; 2.5.6 Alcohol Dehydrogenases (ADH); 2.5.7 Aldehyde Dehydrogenases (ALDH); 2.6 Reduction; 2.6.1 P450, ADH; 2.6.2 NADPH-P450 Reductase; 2.6.3 Aldo-Keto Reductases (AKR); 2.6.4 Quinone Reductase (NQO); 2.6.5 Glutathione Peroxidase (GPX); 2.7 Hydrolysis; 2.7.1 Epoxide Hydrolase; 2.7.2 Esterases and Amidases 2.8 SummaryReferences; 3 Conjugative Metabolism of Drugs; 3.1 UDP-Glucuronosyltransferases; 3.1.1 Location Within the Cell; 3.1.2 Endogenous Substrates; 3.1.3 Enzyme Multiplicity; 3.1.4 Inducibility; 3.1.5 Pharmacogenetics; 3.1.6 Experimental Considerations; 3.1.7 Enzyme Selective Substrates and Inhibitors; 3.1.8 Drug-Drug Interactions and Glucuronidation; 3.1.9 Summary; 3.2 Cytosolic Sulfotransferases; 3.2.1 Cellular Location and Tissue Expression; 3.2.2 The SULT Superfamily of Cytosolic Enzymes; 3.2.3 Inducibility; 3.2.4 SULT Pharmacogenetics 3.2.5 Analytical Detection of Sulfonated Metabolites3.2.6 SULT Inhibitors (Pacifici and Coughtrie, 2005); 3.2.7 Drug-Drug Interactions and Sulfonation; 3.2.8 Summary; 3.3 Glutathione-S-Transferases; 3.3.1 General Overview; 3.3.2 Classification of the GST Enzymes; 3.3.3 Localization and Expression; 3.3.4 Reactions Catalyzed by GSTs; 3.3.5 Regulation of GSTs; 3.3.6 GST Alpha Class; 3.3.7 GST Mu Class; 3.3.8 GST Pi Class; 3.3.9 GST Theta Class; 3.3.10 GST Zeta Class; 3.3.11 Incubation Conditions and Analytical Methods; 3.3.12 Glutathione Conjugate Metabolism (Mercapturic Acid Pathway) References4 Enzyme Kinetics; 4.1 Introduction; 4.2 Enzyme Catalysis; 4.3 Michaelis-Menten Kinetics; 4.3.1 Meanings of K(m), V(max) and Their Clinical Relevance; 4.4 Graphical Kinetic Plots; 4.5 Atypical Kinetics-Allosteric Effects; 4.5.1 Overview of Atypical Kinetic Phenomena; 4.5.2 Homotropic Cooperativity; 4.5.3 Heterotropic Cooperativity; 4.6 Graphical Analysis of Atypical Kinetic Data; 4.7 Enzyme Inhibition Kinetics; 4.7.1 Overview; 4.7.2 Competitive Inhibition; 4.7.3 Mixed Inhibition; 4.7.4 Noncompetitive Inhibition; 4.7.5 Uncompetitive Inhibition 4.7.6 Summary of Effects of Various Inhibition Types of Kinetic Parameters |
Record Nr. | UNINA-9910830456403321 |
Hoboken, N.J., : Wiley-Interscience, c2008 | ||
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Lo trovi qui: Univ. Federico II | ||
|
Drug metabolism in drug design and development [[electronic resource] ] : basic concepts and practice / / edited by Donglu Zhang, Mingshe Zhu, W. Griffith Humphreys |
Pubbl/distr/stampa | Hoboken, N.J., : Wiley-Interscience, c2008 |
Descrizione fisica | 1 online resource (633 p.) |
Disciplina |
615.7
615/.7 |
Altri autori (Persone) |
ZhangDonglu
ZhuMingshe HumphreysW. Griffith |
Soggetto topico |
Drugs - Metabolism
Drugs - Design Drug development |
ISBN |
1-281-09423-4
9786611094232 0-470-19169-4 0-470-19168-6 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
DRUG METABOLISM IN DRUG DESIGN AND DEVELOPMENT; CONTENTS; Preface; Contributors; PART I BASIC CONCEPTS OF DRUG METABOLISM; 1 Overview: Drug Metabolism in the Modern Pharmaceutical Industry; 1.1 Introduction; 1.2 Technology; 1.3 Breadth of Science; 1.3.1 Chemistry; 1.3.2 Enzymology and Molecular Biology; 1.4 Impact of Drug Metabolism on Efficacy and Safety; 1.4.1 Efficacy; 1.4.2 Safety; 1.5 Regulatory Impact and IP Position; 1.6 Summary; References; 2 Oxidative, Reductive, and Hydrolytic Metabolism of Drugs; 2.1 Introduction; 2.2 Nomenclature and Terminology
2.3 General Features of the Enzymes2.4 Fractional Contributions of Different Enzymes; 2.5 Oxidation Enzymes; 2.5.1 Cytochrome P450 (P450, CYP); 2.5.2 Flavin-Containing Monooxygenase (FMO); 2.5.3 Monoamine Oxidase (MAO); 2.5.4 Aldehyde Oxidase and Xanthine Dehydrogenase; 2.5.5 Peroxidases; 2.5.6 Alcohol Dehydrogenases (ADH); 2.5.7 Aldehyde Dehydrogenases (ALDH); 2.6 Reduction; 2.6.1 P450, ADH; 2.6.2 NADPH-P450 Reductase; 2.6.3 Aldo-Keto Reductases (AKR); 2.6.4 Quinone Reductase (NQO); 2.6.5 Glutathione Peroxidase (GPX); 2.7 Hydrolysis; 2.7.1 Epoxide Hydrolase; 2.7.2 Esterases and Amidases 2.8 SummaryReferences; 3 Conjugative Metabolism of Drugs; 3.1 UDP-Glucuronosyltransferases; 3.1.1 Location Within the Cell; 3.1.2 Endogenous Substrates; 3.1.3 Enzyme Multiplicity; 3.1.4 Inducibility; 3.1.5 Pharmacogenetics; 3.1.6 Experimental Considerations; 3.1.7 Enzyme Selective Substrates and Inhibitors; 3.1.8 Drug-Drug Interactions and Glucuronidation; 3.1.9 Summary; 3.2 Cytosolic Sulfotransferases; 3.2.1 Cellular Location and Tissue Expression; 3.2.2 The SULT Superfamily of Cytosolic Enzymes; 3.2.3 Inducibility; 3.2.4 SULT Pharmacogenetics 3.2.5 Analytical Detection of Sulfonated Metabolites3.2.6 SULT Inhibitors (Pacifici and Coughtrie, 2005); 3.2.7 Drug-Drug Interactions and Sulfonation; 3.2.8 Summary; 3.3 Glutathione-S-Transferases; 3.3.1 General Overview; 3.3.2 Classification of the GST Enzymes; 3.3.3 Localization and Expression; 3.3.4 Reactions Catalyzed by GSTs; 3.3.5 Regulation of GSTs; 3.3.6 GST Alpha Class; 3.3.7 GST Mu Class; 3.3.8 GST Pi Class; 3.3.9 GST Theta Class; 3.3.10 GST Zeta Class; 3.3.11 Incubation Conditions and Analytical Methods; 3.3.12 Glutathione Conjugate Metabolism (Mercapturic Acid Pathway) References4 Enzyme Kinetics; 4.1 Introduction; 4.2 Enzyme Catalysis; 4.3 Michaelis-Menten Kinetics; 4.3.1 Meanings of K(m), V(max) and Their Clinical Relevance; 4.4 Graphical Kinetic Plots; 4.5 Atypical Kinetics-Allosteric Effects; 4.5.1 Overview of Atypical Kinetic Phenomena; 4.5.2 Homotropic Cooperativity; 4.5.3 Heterotropic Cooperativity; 4.6 Graphical Analysis of Atypical Kinetic Data; 4.7 Enzyme Inhibition Kinetics; 4.7.1 Overview; 4.7.2 Competitive Inhibition; 4.7.3 Mixed Inhibition; 4.7.4 Noncompetitive Inhibition; 4.7.5 Uncompetitive Inhibition 4.7.6 Summary of Effects of Various Inhibition Types of Kinetic Parameters |
Record Nr. | UNINA-9910840505403321 |
Hoboken, N.J., : Wiley-Interscience, c2008 | ||
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Lo trovi qui: Univ. Federico II | ||
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Drug-like properties [[electronic resource] ] : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di |
Autore | Kerns Edward Harvel |
Pubbl/distr/stampa | Amsterdam ; ; Boston, : Academic Press, c2008 |
Descrizione fisica | 1 online resource (549 p.) |
Disciplina | 615/.19 |
Altri autori (Persone) | DiLi |
Soggetto topico |
Pharmaceutical chemistry
Drugs - Structure-activity relationships Drug development Drugs - Design |
Soggetto genere / forma | Electronic books. |
ISBN |
1-281-76371-3
9786611763718 0-08-095162-7 0-08-055761-9 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
Front Cover; Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization; Copyright Page; Table of Contents; Preface; Dedication; Part 1 Introductory Concepts; Chapter 1 Introduction; Problems; References; Chapter 2 Advantages of Good Drug-like Properties; 2.1 Drug-like Properties Are an Integral Part of Drug Discovery; 2.1.1 Many Properties Are of Interest in Discovery; 2.1.2 Introduction to the Drug Discovery and Development Process; 2.1.3 Development Attrition is Reduced by Improving Drug Properties
2.1.4 Poor Drug Properties Also Cause Discovery Inefficiencies2.1.5 Marginal Drug Properties Cause Inefficiencies During Development; 2.1.6 Poor Properties Can Cause Poor Discovery Research; 2.2 Changing Emphasis on Properties in Discovery; 2.3 Property Profiling in Discovery; 2.4 Drug-like Property Optimization in Discovery; Problems; References; Chapter 3 Barriers to Drug Exposure in Living Systems; 3.1 Introduction to Barriers; 3.2 Drug Dosing; 3.3 Barriers in the Mouth and Stomach; 3.4 Gastrointestinal Tract Barriers; 3.4.1 Permeation of the Gastrointestinal Cellular Membrane 3.4.2 Passive Diffusion at the Molecular Level3.4.3 Metabolism in the Intestine; 3.4.4 Enzymatic Hydrolysis in the Intestine; 3.4.5 Absorption Enhancement in the Intestine; 3.5 Barriers in the Bloodstream; 3.5.1 Plasma Enzyme Hydrolysis; 3.5.2 Plasma Protein Binding; 3.5.3 Red Blood Cell Binding; 3.6 Barriers in the Liver; 3.6.1 Metabolism; 3.6.2 Biliary Excretion; 3.7 Barriers in the Kidney; 3.8 Blood-Tissue Barriers; 3.9 Tissue Distribution; 3.10 Consequences of Chirality on Barriers and Properties; 3.11 Overview of In Vivo Barriers; Problems; References; Part 2 Physicochemical Properties Chapter 4 Rules for Rapid Property Profiling from Structure4.1 Lipinski Rules; 4.2 Veber Rules; 4.3 Other Rules; 4.4 Application of Rules for Compound Assessment; Problems; References; Chapter 5 Lipophilicity; 5.1 Lipophilicity Fundamentals; 5.2 Lipophilicity Effects; 5.3 Lipophilicity Case Studies and Structure Modification; Problems; References; Chapter 6 pKa; 6.1 pKa Fundamentals; 6.2 pKa Effects; 6.3 pKa Case Studies; 6.4 Structure Modification Strategies for pKa; Problems; References; Chapter 7 Solubility; 7.1 Solubility Fundamentals 7.1.1 Solubility Varies with Structure and Physical Conditions7.1.2 Dissolution Rate; 7.1.3 Structural Properties Affect Solubility; 7.1.4 Kinetic and Thermodynamic Solubility; 7.2 Effects of Solubility; 7.2.1 Low Solubility Limits Absorption and Causes Low Oral Bioavailability; 7.2.2 Good Solubility is Essential for IV Formulation; 7.2.3 Acceptance Criteria and Classifications for Solubility; 7.2.4 Molecular Properties for Solubility and Permeability Often are Opposed; 7.3 Effects of Physiology on Solubility and Absorption; 7.3.1 Physiology of the Gastrointestinal Tract 7.3.2 Species Differences in Gastrointestinal Tract |
Record Nr. | UNINA-9910453434903321 |
Kerns Edward Harvel
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Amsterdam ; ; Boston, : Academic Press, c2008 | ||
![]() | ||
Lo trovi qui: Univ. Federico II | ||
|
Drug-like properties : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di |
Autore | Kerns Edward Harvel |
Pubbl/distr/stampa | Amsterdam ; ; Boston : , : Academic Press, , 2008 |
Descrizione fisica | 1 online resource (xix, 526 pages, 2 unnumbered pages of plates) : illustrations (some color) |
Disciplina | 615/.19 |
Altri autori (Persone) | DiLi |
Soggetto topico |
Pharmaceutical chemistry
Drugs - Structure-activity relationships Drug development Drugs - Design |
ISBN |
1-281-76371-3
9786611763718 0-08-095162-7 0-08-055761-9 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
Front Cover; Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization; Copyright Page; Table of Contents; Preface; Dedication; Part 1 Introductory Concepts; Chapter 1 Introduction; Problems; References; Chapter 2 Advantages of Good Drug-like Properties; 2.1 Drug-like Properties Are an Integral Part of Drug Discovery; 2.1.1 Many Properties Are of Interest in Discovery; 2.1.2 Introduction to the Drug Discovery and Development Process; 2.1.3 Development Attrition is Reduced by Improving Drug Properties
2.1.4 Poor Drug Properties Also Cause Discovery Inefficiencies; 2.1.5 Marginal Drug Properties Cause Inefficiencies During Development; 2.1.6 Poor Properties Can Cause Poor Discovery Research; 2.2 Changing Emphasis on Properties in Discovery; 2.3 Property Profiling in Discovery; 2.4 Drug-like Property Optimization in Discovery; Problems; References; Chapter 3 Barriers to Drug Exposure in Living Systems; 3.1 Introduction to Barriers; 3.2 Drug Dosing; 3.3 Barriers in the Mouth and Stomach; 3.4 Gastrointestinal Tract Barriers; 3.4.1 Permeation of the Gastrointestinal Cellular Membrane 3.4.2 Passive Diffusion at the Molecular Level; 3.4.3 Metabolism in the Intestine; 3.4.4 Enzymatic Hydrolysis in the Intestine; 3.4.5 Absorption Enhancement in the Intestine; 3.5 Barriers in the Bloodstream; 3.5.1 Plasma Enzyme Hydrolysis; 3.5.2 Plasma Protein Binding; 3.5.3 Red Blood Cell Binding; 3.6 Barriers in the Liver; 3.6.1 Metabolism; 3.6.2 Biliary Excretion; 3.7 Barriers in the Kidney; 3.8 Blood-Tissue Barriers; 3.9 Tissue Distribution; 3.10 Consequences of Chirality on Barriers and Properties; 3.11 Overview of In Vivo Barriers; Problems; References; Part 2 Physicochemical Properties Chapter 4 Rules for Rapid Property Profiling from Structure; 4.1 Lipinski Rules; 4.2 Veber Rules; 4.3 Other Rules; 4.4 Application of Rules for Compound Assessment; Problems; References; Chapter 5 Lipophilicity; 5.1 Lipophilicity Fundamentals; 5.2 Lipophilicity Effects; 5.3 Lipophilicity Case Studies and Structure Modification; Problems; References; Chapter 6 pKa; 6.1 pKa Fundamentals; 6.2 pKa Effects; 6.3 pKa Case Studies; 6.4 Structure Modification Strategies for pKa; Problems; References; Chapter 7 Solubility; 7.1 Solubility Fundamentals 7.1.1 Solubility Varies with Structure and Physical Conditions; 7.1.2 Dissolution Rate; 7.1.3 Structural Properties Affect Solubility; 7.1.4 Kinetic and Thermodynamic Solubility; 7.2 Effects of Solubility; 7.2.1 Low Solubility Limits Absorption and Causes Low Oral Bioavailability; 7.2.2 Good Solubility is Essential for IV Formulation; 7.2.3 Acceptance Criteria and Classifications for Solubility; 7.2.4 Molecular Properties for Solubility and Permeability Often are Opposed; 7.3 Effects of Physiology on Solubility and Absorption; 7.3.1 Physiology of the Gastrointestinal Tract; 7.3.2 Species Differences in Gastrointestinal Tract |
Record Nr. | UNINA-9910782360503321 |
Kerns Edward Harvel
![]() |
||
Amsterdam ; ; Boston : , : Academic Press, , 2008 | ||
![]() | ||
Lo trovi qui: Univ. Federico II | ||
|
Drug-like properties : concepts, structure design and methods : from ADME to toxicity optimization / / Edward H. Kerns and Li Di |
Autore | Kerns Edward Harvel |
Edizione | [1st ed.] |
Pubbl/distr/stampa | Amsterdam ; ; Boston : , : Academic Press, , 2008 |
Descrizione fisica | 1 online resource (xix, 526 pages, 2 unnumbered pages of plates) : illustrations (some color) |
Disciplina | 615/.19 |
Altri autori (Persone) | DiLi |
Soggetto topico |
Pharmaceutical chemistry
Drugs - Structure-activity relationships Drug development Drugs - Design |
ISBN |
1-281-76371-3
9786611763718 0-08-095162-7 0-08-055761-9 |
Formato | Materiale a stampa ![]() |
Livello bibliografico | Monografia |
Lingua di pubblicazione | eng |
Nota di contenuto |
Front Cover; Drug-like Properties: Concepts, Structure Design and Methods: from ADME to Toxicity Optimization; Copyright Page; Table of Contents; Preface; Dedication; Part 1 Introductory Concepts; Chapter 1 Introduction; Problems; References; Chapter 2 Advantages of Good Drug-like Properties; 2.1 Drug-like Properties Are an Integral Part of Drug Discovery; 2.1.1 Many Properties Are of Interest in Discovery; 2.1.2 Introduction to the Drug Discovery and Development Process; 2.1.3 Development Attrition is Reduced by Improving Drug Properties
2.1.4 Poor Drug Properties Also Cause Discovery Inefficiencies; 2.1.5 Marginal Drug Properties Cause Inefficiencies During Development; 2.1.6 Poor Properties Can Cause Poor Discovery Research; 2.2 Changing Emphasis on Properties in Discovery; 2.3 Property Profiling in Discovery; 2.4 Drug-like Property Optimization in Discovery; Problems; References; Chapter 3 Barriers to Drug Exposure in Living Systems; 3.1 Introduction to Barriers; 3.2 Drug Dosing; 3.3 Barriers in the Mouth and Stomach; 3.4 Gastrointestinal Tract Barriers; 3.4.1 Permeation of the Gastrointestinal Cellular Membrane 3.4.2 Passive Diffusion at the Molecular Level; 3.4.3 Metabolism in the Intestine; 3.4.4 Enzymatic Hydrolysis in the Intestine; 3.4.5 Absorption Enhancement in the Intestine; 3.5 Barriers in the Bloodstream; 3.5.1 Plasma Enzyme Hydrolysis; 3.5.2 Plasma Protein Binding; 3.5.3 Red Blood Cell Binding; 3.6 Barriers in the Liver; 3.6.1 Metabolism; 3.6.2 Biliary Excretion; 3.7 Barriers in the Kidney; 3.8 Blood-Tissue Barriers; 3.9 Tissue Distribution; 3.10 Consequences of Chirality on Barriers and Properties; 3.11 Overview of In Vivo Barriers; Problems; References; Part 2 Physicochemical Properties Chapter 4 Rules for Rapid Property Profiling from Structure; 4.1 Lipinski Rules; 4.2 Veber Rules; 4.3 Other Rules; 4.4 Application of Rules for Compound Assessment; Problems; References; Chapter 5 Lipophilicity; 5.1 Lipophilicity Fundamentals; 5.2 Lipophilicity Effects; 5.3 Lipophilicity Case Studies and Structure Modification; Problems; References; Chapter 6 pKa; 6.1 pKa Fundamentals; 6.2 pKa Effects; 6.3 pKa Case Studies; 6.4 Structure Modification Strategies for pKa; Problems; References; Chapter 7 Solubility; 7.1 Solubility Fundamentals 7.1.1 Solubility Varies with Structure and Physical Conditions; 7.1.2 Dissolution Rate; 7.1.3 Structural Properties Affect Solubility; 7.1.4 Kinetic and Thermodynamic Solubility; 7.2 Effects of Solubility; 7.2.1 Low Solubility Limits Absorption and Causes Low Oral Bioavailability; 7.2.2 Good Solubility is Essential for IV Formulation; 7.2.3 Acceptance Criteria and Classifications for Solubility; 7.2.4 Molecular Properties for Solubility and Permeability Often are Opposed; 7.3 Effects of Physiology on Solubility and Absorption; 7.3.1 Physiology of the Gastrointestinal Tract; 7.3.2 Species Differences in Gastrointestinal Tract |
Record Nr. | UNINA-9910827925703321 |
Kerns Edward Harvel
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Amsterdam ; ; Boston : , : Academic Press, , 2008 | ||
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Lo trovi qui: Univ. Federico II | ||
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