Chemistry and Medicines

Medicinal chemistry incorporates bio-organic chemistry, organic synthetic methods, physical organic chemistry and organic reaction mechanisms. These areas of chemistry are crucial to the design and synthesis of new drugs, both in academia and the pharmaceutical industry. Chemistry and Medicines: An Introductory Text provides a general introduction to this fascinating subject. The first chapters contain a brief historical introduction followed by a description of the chemical features involved in the adsorption, distribution, metabolism and excretion of a drug. The remaining chapters describe the chemistry underlying the design and synthesis of some of the key drugs used to combat some major diseases of the peripheral and central nervous system, infectious diseases and cancers. A glossary and suggestions for further reading complete this textbook. The book is aimed at those studying advanced undergraduate and postgraduate courses in medicinal chemistry.

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.

What is included with this book?

The New copy of this book will include any supplemental materials advertised. Please check the title of the book to determine if it should include any access cards, study guides, lab manuals, CDs, etc.

The Used, Rental and eBook copies of this book are not guaranteed to include any supplemental materials. Typically, only the book itself is included. This is true even if the title states it includes any access cards, study guides, lab manuals, CDs, etc.

FREE SHIPPING

Amazon no longer offers textbook rentals. We do!

Chemistry and Medicines

Summary

Table of Contents

Supplemental Materials