Chemistry and Medicines

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