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Chemistry and Medicines: An Introductory Text Book

Chemistry and Medicines: An Introductory Text
Chemistry and Medicines: An Introductory Text, , Chemistry and Medicines: An Introductory Text has a rating of 4 stars
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Chemistry and Medicines: An Introductory Text, , Chemistry and Medicines: An Introductory Text
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  • Chemistry and Medicines: An Introductory Text
  • Written by author J R Hanson
  • Published by Royal Society of Chemistry, The, October 2006
  • 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 pharmace
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Authors

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


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