The Practice of Medicinal Chemistry

3rd Edition

Print ISBN: 9780123741943
eBook ISBN: 9780080568775
Imprint: Academic Press
Published Date: 24th July 2008
Page Count: 982
125.00 + applicable tax
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The Practice of Medicinal Chemistry fills a gap in the list of available medicinal chemistry literature. It is a single-volume source on the practical aspects of medicinal chemistry. Considered ""the Bible"" by medicinal chemists, the book emphasizes the methods that chemists use to conduct their research and design new drug entities. It serves as a practical handbook about the drug discovery process, from conception of the molecules to drug production.

The first part of the book covers the background of the subject matter, which includes the definition and history of medicinal chemistry, the measurement of biological activities, and the main phases of drug activity. The second part of the book presents the road to discovering a new lead compound and creating a working hypothesis. The main parts of the book discuss the optimization of the lead compound in terms of potency, selectivity, and safety.

The Practice of Medicinal Chemistry can be considered a ""first-read"" or ""bedside book"" for readers who are embarking on a career in medicinal chemistry.

Key Features


  • Focus on chemoinformatics and drug discovery
  • Enhanced pedagogical features
  • New chapters including:
    • Drug absorption and transport
    • Multi-target drugs
  • Updates on hot new areas: NEW! Drug discovery and the latest techniques NEW! How potential drugs can move through the drug discovery/ development phases more quickly NEW! Chemoinformatics


Pharmaceutical researchers in drug discovery, chemists

Table of Contents

Biography Section Editors Contributors Preface to the First Edition Preface to the Second Edition Preface to the Third Edition Part I General Aspects of Medicinal Chemistry

1. A History of Drug Discovery I. Introduction II. Two Hundred Years of Drug Discoveries III. Considerations on Recent Trends in Drug Discovery References 2. Medicinal Chemistry: Definitions and Objectives, Drug Activity Phases, Drug Classification Systems I. Definitions and Objectives II. Drug Activity Phases III. Drug Classification Systems References 3. Measurement and Expression of Drug Effects I. Introduction II. In Vitro Experiments III. Ex Vivo Experiments IV. In Vivo Experiments References 4. Molecular Drug Targets I. Introduction II. Enzymes as Drug Targets III. Membrane Transporters as Drug Targets IV. Voltage-Gated Ion Channels as Drug Targets V. Non-Selective Cation Channels as Drug Targets VI. Direct Ligand-Gated Ion Channels (Receptors with Intrinsic Ion Channel) VII. Receptors with Intrinsic Enzyme Activity VIII. Receptors Coupled to Various Cytosolic Proteins IX. G-Protein-Coupled Receptors X. Nuclear Receptors As Drug Targets References 5. Drug Targets, Target Identification, Validation and Screening I. Introduction II. Improving the Resolution of Disease Etiology III. Biopharmaceutical Therapies IV. Drug Target Identification V. Hit-to-Lead VI. Clinical Biomarkers VII. Conclusions References

Part II Lead Compound Discovery Strategies

6. Strategies in the Search for New Lead Compounds or Original Working Hypotheses I. Introduction II. First Strategy: Analog Design


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© Academic Press 2008
Academic Press
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“A useful, authoritative discussion of the principles and practice of medicinal chemistry... the volume has a useful index, is well produced and is very reasonably priced." - JOURNAL OF MEDICINAL CHEMISTRY