Providing a general introduction to this fascinating subject, this book is aimed at those studying advanced undergraduate and postgraduate courses in medicinal chemistry.
Providing a general introduction to this fascinating subject, this book is aimed at those studying advanced undergraduate and postgraduate courses in medicinal chemistry.Hinweis: Dieser Artikel kann nur an eine deutsche Lieferadresse ausgeliefert werden.
Professor Hanson is Emeritus Professor of Chemistry at the University of Sussex.
Inhaltsangabe
Chapter 1: Introduction 1.1: Aims 1.2: The Classification of Drugs 1.3: Targets for the Medicinal Chemist 1.4: The Stages in the Development of a Drug 1.5: The Synthesis of a Drug 1.6: The History of Medicinal Chemistry Chapter 2: General Principles of Medicinal Chemistry 2.1: Aims 2.2: Administration and Absorption 2.3: The Gastrointestinal Tract 2.4: Other Routes of Administration 2.5: Physico-Chemical Measurements 2.6: Formulation 2.7: Drug Metabolism 2.8: Oxidation by Cytochrome P450s 2.9: The Hydroxylation of Aromatic Rings 2.10: The Hydroxylation of Aliphatic Systems 2.11: The Monoamine Oxidases 2.12: Other Phase One Changes 2.13: Phase Two Changes 2.14: Excretion 2.15: Pro-Drugs 2.16: Quantitative Structure: Activity Relationships 2.17: Hansch QSAR Analyses 2.18: Craig Plots and the Topliss Decision Tree 2.19: Drug: Receptor Interactions Chapter 3: Neurotransmitters as Targets 3.1: Aims 3.2: Introduction 3.3: The Nervous System 3.4: The Neurotransmitters 3.5: Cell-Surface Receptors 3.6: Ion-Channel-Linked Receptors 3.7: Kinase-Linked Receptors 3.8: G-Protein-Linked Receptors 3.9: Agonists and Antagonists 3.10: Acetylcholine 3.11: Neuromuscular Blocking Agents in Surgery 3.12: Muscarinic Agonists 3.13: Local Anaesthetics 3.14: Catecholamines as Neurotransmitters 3.15: The Adrenergic Receptors 3.16: a-Adrenergic Receptor Agonists 3.17: b-Adrenergic Receptor Agonists - The Developmentof Anti-Asthma Drugs 3.18: b1-Adrenergic Antagonists 'b-Blockers' 3.19: The Treatment of Hypertension Chapter 4 Medicinal Chemistry and the Central Nervous System 4.1: Aims 4.2: Introduction 4.3: The Treatment of Neurodegenerative Diseases 4.4: Dopamine Antagonists as Neuroleptic Agents 4.5: Serotonin as a Neurotransmitter 4.6: The Treatment of Depression 4.7: GABA as a Neurotransmitter 4.8: The Treatment of Epilepsy 4.9: Benzodiazepines as Anxiolytic Agents 4.10: Barbiturate Sleeping Tablets 4.11: Opioids as Analgesics Chapter 5: Local and Circulatory Hormone Targets 5.1: Aims 5.2: Introduction 5.3: Histamine as a Target 5.4: Histamine Antagonists in the Treatment of Peptic Ulcers 5.5: The Prostaglandins and Non-Steroidal Anti-Inflammatory Agents 5.6: The Development of Ibuprofen 5.7: The Mechanism of Action of Aspirin 5.8: Medicinal Uses of Prostaglandins 5.9: The Sterols and Steroid Hormones 5.10: The Biosynthesis of the Steroids 5.11: The Control of Cholesterol Biosynthesis 5.12: The Steroidal Anti-Inflammatory Agents 5.13: The Steroidal Oral Contraceptives 5.14: The Role of Nitric Oxide Chapter 6: Anti-infective Agents 6.1: Aims 6.2: Introduction 6.3: Bacterial Diseases 6.4: Antiseptics 6.5: The Sulfonamide Anti-Bacterial Agents 6.6: The Penicillins 6.7: Clavulanic Acid and the Inhibition of b-Lactamases 6.8: The Cephalosporins 6.9: The Mode of Action of the b-Lactam Antibiotics 6.10: Other Antibiotics 6.11: Synthetic Anti-Bacterial Agents 6.12: Anti-Viral Agents 6.13: The Inhibition of Nucleic Acid Biosynthesis 6.14: Inhibitors of Reverse Transcriptase 6.15: Neuraminidase Inhibitors 6.16: The Synthesis of Nucleoside Analogues 6.17: Anti-Fungal Agents 6.18: Ergosterol Biosynthesis Inhibitors 6.19: Other Anti-Fungal Agents 6.20: Parasitic Infections Chapter 7: Cancer Chemotherapy 7.1: Aims 7.2: Introduction 7.3: The Cell Cycle 7.4: Cancer Chemotherapy 7.5: Anti-Metabolites 7.6: Alkylating Agents 7.7: Intercalating Agents 7.8: Anti-Mitotic Agents 7.9: Interference with Selected Developmental Processes 7.10: Monoclonal Antibodies 7.11: Prostate Cancer Further Reading Glossary Subject Index
Chapter 1: Introduction 1.1: Aims 1.2: The Classification of Drugs 1.3: Targets for the Medicinal Chemist 1.4: The Stages in the Development of a Drug 1.5: The Synthesis of a Drug 1.6: The History of Medicinal Chemistry Chapter 2: General Principles of Medicinal Chemistry 2.1: Aims 2.2: Administration and Absorption 2.3: The Gastrointestinal Tract 2.4: Other Routes of Administration 2.5: Physico-Chemical Measurements 2.6: Formulation 2.7: Drug Metabolism 2.8: Oxidation by Cytochrome P450s 2.9: The Hydroxylation of Aromatic Rings 2.10: The Hydroxylation of Aliphatic Systems 2.11: The Monoamine Oxidases 2.12: Other Phase One Changes 2.13: Phase Two Changes 2.14: Excretion 2.15: Pro-Drugs 2.16: Quantitative Structure: Activity Relationships 2.17: Hansch QSAR Analyses 2.18: Craig Plots and the Topliss Decision Tree 2.19: Drug: Receptor Interactions Chapter 3: Neurotransmitters as Targets 3.1: Aims 3.2: Introduction 3.3: The Nervous System 3.4: The Neurotransmitters 3.5: Cell-Surface Receptors 3.6: Ion-Channel-Linked Receptors 3.7: Kinase-Linked Receptors 3.8: G-Protein-Linked Receptors 3.9: Agonists and Antagonists 3.10: Acetylcholine 3.11: Neuromuscular Blocking Agents in Surgery 3.12: Muscarinic Agonists 3.13: Local Anaesthetics 3.14: Catecholamines as Neurotransmitters 3.15: The Adrenergic Receptors 3.16: a-Adrenergic Receptor Agonists 3.17: b-Adrenergic Receptor Agonists - The Developmentof Anti-Asthma Drugs 3.18: b1-Adrenergic Antagonists 'b-Blockers' 3.19: The Treatment of Hypertension Chapter 4 Medicinal Chemistry and the Central Nervous System 4.1: Aims 4.2: Introduction 4.3: The Treatment of Neurodegenerative Diseases 4.4: Dopamine Antagonists as Neuroleptic Agents 4.5: Serotonin as a Neurotransmitter 4.6: The Treatment of Depression 4.7: GABA as a Neurotransmitter 4.8: The Treatment of Epilepsy 4.9: Benzodiazepines as Anxiolytic Agents 4.10: Barbiturate Sleeping Tablets 4.11: Opioids as Analgesics Chapter 5: Local and Circulatory Hormone Targets 5.1: Aims 5.2: Introduction 5.3: Histamine as a Target 5.4: Histamine Antagonists in the Treatment of Peptic Ulcers 5.5: The Prostaglandins and Non-Steroidal Anti-Inflammatory Agents 5.6: The Development of Ibuprofen 5.7: The Mechanism of Action of Aspirin 5.8: Medicinal Uses of Prostaglandins 5.9: The Sterols and Steroid Hormones 5.10: The Biosynthesis of the Steroids 5.11: The Control of Cholesterol Biosynthesis 5.12: The Steroidal Anti-Inflammatory Agents 5.13: The Steroidal Oral Contraceptives 5.14: The Role of Nitric Oxide Chapter 6: Anti-infective Agents 6.1: Aims 6.2: Introduction 6.3: Bacterial Diseases 6.4: Antiseptics 6.5: The Sulfonamide Anti-Bacterial Agents 6.6: The Penicillins 6.7: Clavulanic Acid and the Inhibition of b-Lactamases 6.8: The Cephalosporins 6.9: The Mode of Action of the b-Lactam Antibiotics 6.10: Other Antibiotics 6.11: Synthetic Anti-Bacterial Agents 6.12: Anti-Viral Agents 6.13: The Inhibition of Nucleic Acid Biosynthesis 6.14: Inhibitors of Reverse Transcriptase 6.15: Neuraminidase Inhibitors 6.16: The Synthesis of Nucleoside Analogues 6.17: Anti-Fungal Agents 6.18: Ergosterol Biosynthesis Inhibitors 6.19: Other Anti-Fungal Agents 6.20: Parasitic Infections Chapter 7: Cancer Chemotherapy 7.1: Aims 7.2: Introduction 7.3: The Cell Cycle 7.4: Cancer Chemotherapy 7.5: Anti-Metabolites 7.6: Alkylating Agents 7.7: Intercalating Agents 7.8: Anti-Mitotic Agents 7.9: Interference with Selected Developmental Processes 7.10: Monoclonal Antibodies 7.11: Prostate Cancer Further Reading Glossary Subject Index
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