Table of Contents

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

About the Author

Professor Hanson is Emeritus Professor of Chemistry at the University of Sussex.

Reviews

Examples, exemplify the approaches and methodology that are peculiar to medicinal chemistry.
*Chemistry World, June 2007, p65 (Michael Waring)*

Illustrates the drug development process through the thoughts of medicinal or organic synthesis chemists, and is a must read for all biochemists in the drug development sector. Destined for undergraduate chemists and biochemists, the book also offers general consultancy for post graduate and professional drug development research scientists.....each chapter includes a brief, developmental history and synthesis of the most popular drugs.Development and discovery of antiseptics such as Dettol, penicillins, ?-lactam antibiotics and AZT is most interesting. Cancer chemotherapy and the use of monoclonal antibodies are well covered in this introductory text. Then the big medical challenge: parasitic infections.
*Chemistry & Industry, 13 August 2007, (Mary Nnankya)*

There are some science books that when reviewed you would be happy to lend out to colleagues while there are others that remain jealously guarded in a drawer. This book falls into the latter category.The content is based upon short medicinal chemistry lecture courses which have been given to students on summer schools.......students know medicinal chemistry is important and what they really need is an easy to read reference text. This is that book and I'm willing to bet that they won't be lending it out either.
*Physical Sciences Educational Reviews, Volume 8, Issue 1 (Elizabeth Barron)*

A highly readable book which covers all of the main types of drugs.....history of drug discovery is excellent......an excellent introduction to all classes of drugs.
*Education in Chemistry, 2007, (John Mann)*