Medicinal Chemistry: An Introduction / Edition 2

Hardcover (Print)
Buy New
Buy New from
Used and New from Other Sellers
Used and New from Other Sellers
from $27.99
Usually ships in 1-2 business days
(Save 85%)
Other sellers (Hardcover)
  • All (9) from $27.99   
  • New (3) from $150.20   
  • Used (6) from $27.99   


Medicinal Chemistry: An Introduction, Second Edition provides a comprehensive, balanced introduction to this evolving and multidisciplinary area of research. Building on the success of the First Edition, this edition has been completely revised and updated to include the latest developments in the field.

Written in an accessible style, Medicinal Chemistry: An Introduction, Second Edition carefully explains fundamental principles, assuming little in the way of prior knowledge. The book focuses on the chemical principles used for drug discovery and design covering physiology and biology where relevant. It opens with a broad overview of the subject with subsequent chapters examining topics in greater depth.

From the reviews of the First Edition:

"It contains a wealth of information in a compact form" ANGEWANDTE CHEMIE, INTERNATIONAL EDITION

"Medicinal Chemistry is certainly a text I would chose to teach from for undergraduates. It fills a unique niche in the market place." PHYSICAL SCIENCES AND EDUCATIONAL REVIEWS

Read More Show Less

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)
Read More Show Less

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

Read More Show Less

Table of Contents

Preface to the First Edition.

Preface to the Second Edition.



1 An introduction to drugs, their action and discovery.

1.1 Introduction.

1.2 What are drugs and why do we need new ones? 

1.3 Drug discovery and design: a historical outline.

1.4 Leads and analogues: some desirable properties.

1.5 Sources of leads and drugs.

1.6 Methods and routes of administration: the pharmaceutical phase.

1.7 Introduction to drug action.

1.8 Classification of drugs.

1.9 Questions.

2 Drug structure and solubility.

2.1 Introduction.

2.2 Structure.

2.3 Stereochemistry and drug design.

2.3.1 Structurally rigid groups.

2.3.2 Conformation.

2.3.3 Configuration.

2.4 Solubility.

2.4.1 Solubility and the physical nature of the solute.

2.5 Solutions.

2.6 The importance of water solubility.

2.7 Solubility and the structure of the solute.

2.8 Salt formation.

2.9 The incorporation of water solubilising groups in a structure.

2.10 Formulation methods of improving water solubility.

2.11 The effect of pH on the solubility of acidic and basic drugs.

2.12 Partition.

2.13 Surfactants and amphiphiles.

2.14 Questions.

3 Structure–activity and quantitative structure relationships.

3.1 Introduction.

3.2 Structure–activity relationship (SAR).

3.3 Changing size and shape.

3.4 Introduction of new substituents.

3.5 Changing the existing substituents of a lead.

3.6 Case study: a SAR investigation to discover potent geminal bisphosphonates.

3.7 Quantitative structure–activity relationship (QSAR).

3.8 Questions.

4 Computer-aided drug design.

4.1 Introduction.

4.1.1 Models.

4.2 Molecular mechanics.

4.3 Molecular dynamics.

4.4 Quantum mechanics.

4.5 Docking.

4.6 Comparing three-dimensional structures by the use of overlays.

4.7 Pharmacophores and some of their uses.

4.8 Modelling protein structures.

4.9 Three-dimensional QSAR.

4.10 Other uses of computers in drug discovery.

4.11 Questions.

5 Combinatorial chemistry.

5.1 Introduction.

5.2 The solid support method.

5.3 Encoding methods.

5.4 Combinatorial synthesis in solution.

5.5 Deconvolution.

5.6 High-throughput screening (HTS).

5.7 Automatic methods of library generation and analysis.

5.8 Questions.

6 Drugs from natural sources.

6.1 Introduction.

6.2 Bioassays.

6.3 Dereplication.

6.4 Structural analysis of the isolated substance.

6.5 Active compound development.

6.6 Extraction procedures.

6.7 Fractionation methods.

6.8 Case history: the story of Taxol.

6.9 Questions.

7 Biological membranes.

7.1 Introduction.

7.2 The plasma membrane.

7.3 The transfer of species through cell membranes.

7.4 Drug action that affects the structure of cell membranes and walls.

7.5 Questions.

8 Receptors and messengers.

8.1 Introduction.

8.2 The chemical nature of the binding of ligands to receptors.

8.3 Structure and classification of receptors.

8.4 General mode of operation.

8.5 Ligand–response relationships.

8.6 Ligand–receptor theories.

8.7 Drug action and design.

8.8 Questions.

9 Enzymes.

9.1 Introduction.

9.2 Classification and nomenclature.

9.3 Active sites and catalytic action.

9.4 Regulation of enzyme activity.

9.5 The specific nature of enzyme action.

9.6 The mechanisms of enzyme action.

9.7 The general physical factors affecting enzyme action.

9.8 Enzyme kinetics.

9.9 Enzyme inhibitors.

9.10 Transition state inhibitors.

9.11 Enzymes and drug design: some general considerations.

9.12 Examples of drugs used as enzyme inhibitors.

9.13 Enzymes and drug resistance.

9.14 Ribozymes.

9.15 Questions.

10 Nucleic acids.

10.1 Introduction.

10.2 Deoxyribonucleic acid (DNA).

10.3 The general functions of DNA.

10.4 Genes.

10.5 Replication.

10.6 Ribonucleic acid (RNA).

10.7 Messenger RNA (mRNA).

10.8 Transfer RNA (tRNA).

10.9 Ribosomal RNA (rRNA).

10.10 Protein synthesis.

10.11 Protein synthesis in prokaryotic and eukaryotic cells.

10.12 Bacterial protein synthesis inhibitors (antimicrobials).

10.13 Drugs that target nucleic acids.

10.14 Viruses.

10.15 Recombinant DNA technology (genetic engineering).

10.16 Questions.

11 Pharmacokinetics.

11.1 Introduction.

11.2 Drug concentration analysis and its therapeutic significance.

11.3 Pharmacokinetic models.

11.4 Intravascular administration.

11.5 Extravascular administration.

11.6 The use of pharmacokinetics in drug design.

11.7 Extrapolation of animal experiments to humans.

11.8 Questions.

12 Drug metabolism.

12.1 Introduction.

12.2 Secondary pharmacological implications of metabolism.

12.2.4 Toxic metabolites.

12.3 Sites of action.

12.4 Phase I metabolic reactions.

12.5 Examples of Phase I metabolic reactions.

12.6 Phase II metabolic routes.

12.7 Pharmacokinetics of metabolites.

12.8 Drug metabolism and drug design.

12.9 Prodrugs.

12.10 Questions.

13 Complexes and chelating agents.

13.1 Introduction.

13.2 The shapes and structures of complexes.

13.3 Metal–ligand affinities.

13.4 The general roles of metal complexes in biological processes.

13.5 Therapeutic uses.

13.6 Drug action and metal chelation.

13.7 Questions.

14 Nitric oxide.

14.1 Introduction.

14.2 The structure of nitric oxide.

14.3 The chemical properties of nitric oxide.

14.4 The cellular production and role of nitric oxide.

14.5 The role of nitric oxide in physiological and pathophysiological states.

14.6 Therapeutic possibilities.

14.7 Questions.

15 An introduction to drug and analogue synthesis.

15.1 Introduction.

15.2 Some general considerations.

15.3 Asymmetry in syntheses.

15.4 Designing organic syntheses.

15.5 Partial organic synthesis of xenobiotics.

15.6 Questions.

16 Drug development and production.

16.1 Introduction.

16.2 Chemical development.

16.3 Pharmacological and toxicological testing.

16.4 Drug metabolism and pharmacokinetics.

16.5 Formulation development.

16.6 Production and quality control.

16.7 Patent protection.

16.8 Regulation.

16.9 Questions.

Selected further reading.

Answers to questions.


Read More Show Less

Customer Reviews

Be the first to write a review
( 0 )
Rating Distribution

5 Star


4 Star


3 Star


2 Star


1 Star


Your Rating:

Your Name: Create a Pen Name or

Barnes & Review Rules

Our reader reviews allow you to share your comments on titles you liked, or didn't, with others. By submitting an online review, you are representing to Barnes & that all information contained in your review is original and accurate in all respects, and that the submission of such content by you and the posting of such content by Barnes & does not and will not violate the rights of any third party. Please follow the rules below to help ensure that your review can be posted.

Reviews by Our Customers Under the Age of 13

We highly value and respect everyone's opinion concerning the titles we offer. However, we cannot allow persons under the age of 13 to have accounts at or to post customer reviews. Please see our Terms of Use for more details.

What to exclude from your review:

Please do not write about reviews, commentary, or information posted on the product page. If you see any errors in the information on the product page, please send us an email.

Reviews should not contain any of the following:

  • - HTML tags, profanity, obscenities, vulgarities, or comments that defame anyone
  • - Time-sensitive information such as tour dates, signings, lectures, etc.
  • - Single-word reviews. Other people will read your review to discover why you liked or didn't like the title. Be descriptive.
  • - Comments focusing on the author or that may ruin the ending for others
  • - Phone numbers, addresses, URLs
  • - Pricing and availability information or alternative ordering information
  • - Advertisements or commercial solicitation


  • - By submitting a review, you grant to Barnes & and its sublicensees the royalty-free, perpetual, irrevocable right and license to use the review in accordance with the Barnes & Terms of Use.
  • - Barnes & reserves the right not to post any review -- particularly those that do not follow the terms and conditions of these Rules. Barnes & also reserves the right to remove any review at any time without notice.
  • - See Terms of Use for other conditions and disclaimers.
Search for Products You'd Like to Recommend

Recommend other products that relate to your review. Just search for them below and share!

Create a Pen Name

Your Pen Name is your unique identity on It will appear on the reviews you write and other website activities. Your Pen Name cannot be edited, changed or deleted once submitted.

Your Pen Name can be any combination of alphanumeric characters (plus - and _), and must be at least two characters long.

Continue Anonymously

    If you find inappropriate content, please report it to Barnes & Noble
    Why is this product inappropriate?
    Comments (optional)