Chemistry and Medicines

by
Edition: 1st
Format: Hardcover
Pub. Date: 2006-10-10
Publisher(s): Royal Society of Chemistry
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Summary

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.

Table of Contents

Introductionp. 1
Aimsp. 1
The Classification of Drugsp. 1
Targets for the Medicinal Chemistp. 2
Hormones as Targetsp. 2
Cellular Structures as Targetsp. 4
The Stages in the Development of a Drugp. 5
The Synthesis of a Drugp. 6
The History of Medicinal Chemistryp. 8
General Principles of Medicinal Chemistryp. 20
Aimsp. 20
Administration and Absorptionp. 20
The Gastrointestinal Tractp. 21
Other Routes of Administrationp. 23
Physico-Chemical Measurementsp. 23
Formulationp. 24
Drug Metabolismp. 25
Oxidation by Cytochrome P[subscript 450]sp. 26
The Hydroxylation of Aromatic Ringsp. 27
The Hydroxylation of Aliphatic Systemsp. 29
The Monoamine Oxidasesp. 30
Other Phase One Changesp. 31
Phase Two Changesp. 32
Excretionp. 33
Pro-Drugsp. 33
Quantitative Structure: Activity Relationshipsp. 35
Hansch QSAR Analysesp. 36
Craig Plots and the Topliss Decision Treep. 38
Drug: Receptor Interactionsp. 39
Neurotransmitters as Targetsp. 41
Aimsp. 41
Introductionp. 41
The Nervous Systemp. 42
The Neurotransmittersp. 44
Cell-Surface Receptorsp. 45
Ion-Channel-Linked Receptorsp. 45
Kinase-Linked Receptorsp. 45
G-Protein-Linked Receptorsp. 46
Agonists and Antagonistsp. 48
Acetylcholinep. 48
Neuromuscular Blocking Agents in Surgeryp. 49
Muscarinic Agonistsp. 51
Local Anaestheticsp. 52
Catecholamines as Neurotransmittersp. 53
The Adrenergic Receptorsp. 55
[alpha]-Adrenergic Receptor Agonistsp. 55
[beta]-Adrenergic Receptor Agonists - The Development of Anti-Asthma Drugsp. 56
[beta1]-Adrenergic Antagonists '[Beta]-Blockers'p. 59
The Treatment of Hypertensionp. 61
Medicinal Chemistry and the Central Nervous Systemp. 64
Aimsp. 64
Introductionp. 64
The Treatment of Neurodegenerative Diseasesp. 66
Alzheimer's Diseasep. 66
Parkinson's Diseasep. 67
Dopamine Antagonists as Neuroleptic Agentsp. 70
Serotonin as a Neurotransmitterp. 72
The Treatment of Depressionp. 73
GABA as a Neurotransmitterp. 76
The Treatment of Epilepsyp. 77
Benzodiazepines as Anxiolytic Agentsp. 78
Barbiturate Sleeping Tabletsp. 80
Opioids as Analgesicsp. 81
Local and Circulatory Hormone Targetsp. 85
Aimsp. 85
Introductionp. 85
Histamine as a Targetp. 86
Histamine Antagonists in the Treatment of Peptic Ulcersp. 87
The Prostaglandins and Non-Steroidal Anti-Inflammatory Agentsp. 90
The Development of Ibuprofenp. 92
The Mechanism of Action of Aspirinp. 94
Medicinal Uses of Prostaglandinsp. 95
The Sterols and Steroid Hormonesp. 96
The Biosynthesis of the Steroidsp. 98
The Control of Cholesterol Biosynthesisp. 100
The Steroidal Anti-Inflammatory Agentsp. 101
The Steroidal Oral Contraceptivesp. 103
The Role of Nitric Oxidep. 104
Anti-infective Agentsp. 105
Aimsp. 105
Introductionp. 105
Bacterial Diseasesp. 106
Antisepticsp. 107
The Sulfonamide Anti-Bacterial Agentsp. 108
The Penicillinsp. 111
Semi-Synthetic Penicillinsp. 114
Clavulanic Acid and the Inhibition of [beta]-Lactamasesp. 114
The Cephalosporinsp. 115
The Mode of Action of the [beta]-Lactam Antibioticsp. 115
Other Antibioticsp. 117
Synthetic Anti-Bacterial Agentsp. 118
Anti-Viral Agentsp. 118
Viral Diseasesp. 118
Viral Structure and Replicationp. 119
Targets for Anti-Viral Agentsp. 120
The Inhibition of Nucleic Acid Biosynthesisp. 120
Inhibitors of Reverse Transcriptasep. 121
Neuraminidase Inhibitorsp. 122
The Synthesis of Nucleoside Analoguesp. 122
Anti-Fungal Agentsp. 124
Ergosterol Biosynthesis Inhibitorsp. 124
Other Anti-Fungal Agentsp. 126
Parasitic Infectionsp. 126
The Treatment of Malariap. 126
Cancer Chemotherapyp. 129
Aimsp. 129
Introductionp. 129
The Cell Cyclep. 129
Cancer Chemotherapyp. 131
Anti-Metabolitesp. 131
Alkylating Agentsp. 134
Intercalating Agentsp. 137
Anti-Mitotic Agentsp. 138
Interference with Selected Developmental Processesp. 138
The Treatment of Breast Cancerp. 138
Monoclonal Antibodiesp. 140
Prostate Cancerp. 141
Further Readingp. 142
Glossaryp. 144
Subject Indexp. 151
Table of Contents provided by Ingram. All Rights Reserved.

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