Medicinal Chemistry: An Introduction [Hardcover]
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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
- Hardcover: 646 pages
- Publisher: Wiley-Interscience; 2 edition (January 22, 2008)
- Language: English
- ISBN-10: 0470025972
- ISBN-13: 978-0470025970
- Product Dimensions: 9.8 x 7.7 x 1.6 inches
- Shipping Weight: 3 pounds (View shipping rates and policies)
- Amazon Best Sellers Rank: #2,860,600 in Books (See Top 100 in Books)
Preface to the Second Edition.
Acknowledgements.
Abbreviations.
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.
Index.
As an undergraduate text for medicinal chemistry, I think this book is the best in the market. It's appropriate for students who have only had two semesters of organic chemistry. The layout is logical. Aside from chapter 7 (chelating agents), the first nine chapters are at least decent and mostly very good. Chapter 10 (nucleic acids) and 11 (nitric oxide) probably belong more in a biochem text than a med chem book. Chapter 12 (organic synthesis) is well out of the scope of this book and falls flat.By A Customer
The book has a huge number of errors. Most of which are in the chemical figures and will not bother anyone unless they like looking at structures. Some of the errors involve the mathematic equations and could cause trouble for a student who isn't paying attention.
The only major complaint I have about the book is that chapter 5 (pharmacokinetics) is almost completely devoid of units on the variables in the equations and graphs. Proper use of units would greatly help a student in learning material in this chapter.
While not perfect, this book is very good for a junior/senior upper-level chemistry course.
This textbook by Thomas is a very big disappointment to me. I am still trying to see how so little useful information can be spread over a vast 620 pages. The subtitle "An introduction" is one thing, but for the author to spend so much time discussing background without giving precise information about how the molecules act as drugs is unfortunate. In so many areas, it is just a waste of the students' time. It has poor illustrations too. The book is inexpensive, but I would rather pay more for a book that I could actually learn some interesting information about. If you wish to learn medicinal chemistry, you need a better book than this. This book give almost no insight in the strategies that a medicinal chemist actually uses to design drugs. Fortunately, there are some very good books out there today. My three favorite MedChem books are those written by: Patrick, Silverman, and Sneader....in that order. Nogrady is also a good book but it suffers from the opposite extreme that this book by Thomas does (it has too many specifics and not enough background).By bro
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