
Chemistry and Medicines
by Hanson, James R.Buy New
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Summary
Table of Contents
Introduction | p. 1 |
Aims | p. 1 |
The Classification of Drugs | p. 1 |
Targets for the Medicinal Chemist | p. 2 |
Hormones as Targets | p. 2 |
Cellular Structures as Targets | p. 4 |
The Stages in the Development of a Drug | p. 5 |
The Synthesis of a Drug | p. 6 |
The History of Medicinal Chemistry | p. 8 |
General Principles of Medicinal Chemistry | p. 20 |
Aims | p. 20 |
Administration and Absorption | p. 20 |
The Gastrointestinal Tract | p. 21 |
Other Routes of Administration | p. 23 |
Physico-Chemical Measurements | p. 23 |
Formulation | p. 24 |
Drug Metabolism | p. 25 |
Oxidation by Cytochrome P[subscript 450]s | p. 26 |
The Hydroxylation of Aromatic Rings | p. 27 |
The Hydroxylation of Aliphatic Systems | p. 29 |
The Monoamine Oxidases | p. 30 |
Other Phase One Changes | p. 31 |
Phase Two Changes | p. 32 |
Excretion | p. 33 |
Pro-Drugs | p. 33 |
Quantitative Structure: Activity Relationships | p. 35 |
Hansch QSAR Analyses | p. 36 |
Craig Plots and the Topliss Decision Tree | p. 38 |
Drug: Receptor Interactions | p. 39 |
Neurotransmitters as Targets | p. 41 |
Aims | p. 41 |
Introduction | p. 41 |
The Nervous System | p. 42 |
The Neurotransmitters | p. 44 |
Cell-Surface Receptors | p. 45 |
Ion-Channel-Linked Receptors | p. 45 |
Kinase-Linked Receptors | p. 45 |
G-Protein-Linked Receptors | p. 46 |
Agonists and Antagonists | p. 48 |
Acetylcholine | p. 48 |
Neuromuscular Blocking Agents in Surgery | p. 49 |
Muscarinic Agonists | p. 51 |
Local Anaesthetics | p. 52 |
Catecholamines as Neurotransmitters | p. 53 |
The Adrenergic Receptors | p. 55 |
[alpha]-Adrenergic Receptor Agonists | p. 55 |
[beta]-Adrenergic Receptor Agonists - The Development of Anti-Asthma Drugs | p. 56 |
[beta1]-Adrenergic Antagonists '[Beta]-Blockers' | p. 59 |
The Treatment of Hypertension | p. 61 |
Medicinal Chemistry and the Central Nervous System | p. 64 |
Aims | p. 64 |
Introduction | p. 64 |
The Treatment of Neurodegenerative Diseases | p. 66 |
Alzheimer's Disease | p. 66 |
Parkinson's Disease | p. 67 |
Dopamine Antagonists as Neuroleptic Agents | p. 70 |
Serotonin as a Neurotransmitter | p. 72 |
The Treatment of Depression | p. 73 |
GABA as a Neurotransmitter | p. 76 |
The Treatment of Epilepsy | p. 77 |
Benzodiazepines as Anxiolytic Agents | p. 78 |
Barbiturate Sleeping Tablets | p. 80 |
Opioids as Analgesics | p. 81 |
Local and Circulatory Hormone Targets | p. 85 |
Aims | p. 85 |
Introduction | p. 85 |
Histamine as a Target | p. 86 |
Histamine Antagonists in the Treatment of Peptic Ulcers | p. 87 |
The Prostaglandins and Non-Steroidal Anti-Inflammatory Agents | p. 90 |
The Development of Ibuprofen | p. 92 |
The Mechanism of Action of Aspirin | p. 94 |
Medicinal Uses of Prostaglandins | p. 95 |
The Sterols and Steroid Hormones | p. 96 |
The Biosynthesis of the Steroids | p. 98 |
The Control of Cholesterol Biosynthesis | p. 100 |
The Steroidal Anti-Inflammatory Agents | p. 101 |
The Steroidal Oral Contraceptives | p. 103 |
The Role of Nitric Oxide | p. 104 |
Anti-infective Agents | p. 105 |
Aims | p. 105 |
Introduction | p. 105 |
Bacterial Diseases | p. 106 |
Antiseptics | p. 107 |
The Sulfonamide Anti-Bacterial Agents | p. 108 |
The Penicillins | p. 111 |
Semi-Synthetic Penicillins | p. 114 |
Clavulanic Acid and the Inhibition of [beta]-Lactamases | p. 114 |
The Cephalosporins | p. 115 |
The Mode of Action of the [beta]-Lactam Antibiotics | p. 115 |
Other Antibiotics | p. 117 |
Synthetic Anti-Bacterial Agents | p. 118 |
Anti-Viral Agents | p. 118 |
Viral Diseases | p. 118 |
Viral Structure and Replication | p. 119 |
Targets for Anti-Viral Agents | p. 120 |
The Inhibition of Nucleic Acid Biosynthesis | p. 120 |
Inhibitors of Reverse Transcriptase | p. 121 |
Neuraminidase Inhibitors | p. 122 |
The Synthesis of Nucleoside Analogues | p. 122 |
Anti-Fungal Agents | p. 124 |
Ergosterol Biosynthesis Inhibitors | p. 124 |
Other Anti-Fungal Agents | p. 126 |
Parasitic Infections | p. 126 |
The Treatment of Malaria | p. 126 |
Cancer Chemotherapy | p. 129 |
Aims | p. 129 |
Introduction | p. 129 |
The Cell Cycle | p. 129 |
Cancer Chemotherapy | p. 131 |
Anti-Metabolites | p. 131 |
Alkylating Agents | p. 134 |
Intercalating Agents | p. 137 |
Anti-Mitotic Agents | p. 138 |
Interference with Selected Developmental Processes | p. 138 |
The Treatment of Breast Cancer | p. 138 |
Monoclonal Antibodies | p. 140 |
Prostate Cancer | p. 141 |
Further Reading | p. 142 |
Glossary | p. 144 |
Subject Index | p. 151 |
Table of Contents provided by Ingram. All Rights Reserved. |
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