Medicinal Chemistry: An Introduction / Edition 2

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Medicinal Chemistry: An Introduction, provides a comprehensive, balanced introduction to this exciting, evolving and multi-disciplinary field. Written in an accessible and readable style, this text carefully explains fundamental principles, assuming little prior knowledge of medicinal chemistry and keeps the approach as simple as possible. Focusing on the chemical principles used for drug discovery and design, it also covers human biology where relevant. The first chapter gives a broad overview of the subject with subsequent chapters examining topics in greater depth. The approach to medicinal chemistry is kept as simple as possible. Each chapter has a summary of its contents, self-assessment questions, numerous examples and applications. * Provides a comprehensive introduction to the field and written in an accessible and readable style * Assumes little prior knowledge of biology and a knowledge of chemistry to first year degree level * Includes examples, applications, problems and summary sections in each chapter This will be an invaluable introduction to students of chemistry, medicinal and pharmaceutical chemistry, pharmacy and pharmacology whose courses include medicinal chemistry units.
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Editorial Reviews

From the Publisher
"The many strengths of this introductory text include its seamless integration of biochemistry and pharmacology to direct drug discovery." (Journal of Medicinal Chemistry, September 2008)
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Product Details

  • ISBN-13: 9780470025970
  • Publisher: Wiley
  • Publication date: 1/18/2008
  • Edition number: 2
  • Pages: 646
  • Product dimensions: 7.70 (w) x 9.94 (h) x 1.59 (d)

Meet the Author

Dr Gareth Thomas. The University of Portsmouth, UK

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Table of Contents

Chapter 1:Introduction
What are drugs and why do we need new ones?
Drug discovery and design, a historical outline
Methods and routes of administration, the pharmaceutical phase
Introduction to drug action
Classification of drugs
Drug Stability
Sources of Drugs
Drug development and production
Chapter 2: Drug Discovery By Design
Stereochemistry and drug design
Structure-activity relationships (SAR)
Quantitative structure-activity relationships (QSAR)
Computer-aided drug design
Combinatorial chemistry
Chapter 3: Drug solubility
The structure of bulk liquids
Solubility and the structure of the solute
Salt formation
The incorporation of water-solubilising groups in a structure
Formulation methods of improving water solubility
The effect of the pH on the solubility of acidic and basic drugs
Surfactants, structure and action
Chapter 4: Biological membranes
The plasma membrane
The transfer of species through cell membranes
Drug action that affects the structure of cell membranes and walls
Chapter 5: Pharmacokinetics
Pharmacokinetic models
Intravascular administration
Extravascular administration
The use of pharmacokinetics in drug design
Extraploation of animal experiments to humans
Chapter 6 - Enzymes
Classification and nomenclature
Active sites and catalytic action
Regulation of enzyme activity
The specific nature of enzyme action
The mechanisms of enzyme action
The generalphysical factors affecting enzyme action
Enzyme kinetics
Enzyme inhibitors
Transition state inhibitors
Enzymes and drug design: some general considerations
Examples of drugs used as enzyme inhibitors
Chapter 7: Complexes and chelating agents
The shapes and structures of complexes
The general roles of metal complexes in biological processes
Therapeutic uses
Drug action and metal chelation
Chapter 8: Receptors and messengers
The bonding of ligands to receptors
Structure and classification of receptors
General mode of operation
Ligand-response relationships
Drug action and design
Chapter 9: Drug Metabolism
Secondary pharmacological implications of metabolism
Sites of action
Phase I metabolic reactions
Phase II metabolic routes
Pharmacokinetics of metabolites
Drug metabolism and drug design
Chapter 10: Nucleic acids
Deoxyribonucleic acids (DNA)
The general functions of DNA
Ribonucleic acids (RNA)
Messenger RNA (mRNA)
Transfer RNA (tRNA)
Ribosomal RNA (rRNA)
Protein synthesis
Protein synthesis in prokaryotic and eukaryotic cells
Bacterial protein synthesis inhibitors (antimicrobials)
Drugs that target nucleic acids
Recombinant DNA (genetic engineering)
Chaper 11: Nitric oxide
The structure of nitric oxide
The chemical properties of nitric oxide
The cellular production and role of nitric oxide
The role of nitric oxide in physiological and pathophysiological states
Therapeutic possibilities
Chapter 12: An introduction to organic drug and analogue synthesis
Some general considerations
Asymmetry in syntheses
Designing organic sysntheses
Partial organic synthesisn of xenobiotics

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