List of Medicinal Chemistry Books

By: Pharma Tips | Views: 85855 | Date: 18-Feb-2013

Medicinal Chemistry is a discipline with a traditional focus on organic synthetic chemistry with the broad goals of drug discovery and optimization. The Department of Medicinal Chemistry at the University of Washington, since its inception in 1980, has always departed somewhat from this tradition given the focus of many of its faculty on the research areas of mechanistic drug metabolism, toxicology and bioanalytical chemistry. In recent years research activities in the Department have been broadened further

List of Medicinal Chemistry Books

Medicinal Books

Welcome to Medicinal Chemistry

Medicinal Chemistry is a discipline with a traditional focus on organic synthetic chemistry with the broad goals of drug discovery and optimization. The Department of Medicinal Chemistry at the University of Washington, since its inception in 1980, has always departed somewhat from this tradition given the focus of many of its faculty on the research areas of mechanistic drug metabolism, toxicology and bioanalytical chemistry. In recent years research activities in the Department have been broadened further by the addition of several faculty members with expertise in the areas of biological mass spectrometry and biophysical virology.

Analogue-based Drug Discovery

J. Fischer, C. R. Ganellin

Hardcover, 575 Pages
1st Edition, 2006
ISBN: 3-527-31257-9


The first authoritative overview of past and current strategies for successful drug development by analog generation, this unique resource spans all important drug classes and all major therapeutic fields, including histamine antagonists, ACE inhibitors, beta blockers, opioids, quinolone antibiotics, steroids and anticancer platinum compounds.

Of the 19 analog classes presented in detail, 9 are described by the scientists who discoverd them.
The book includes a table of the most successful drug analogs as based on the IMS ranking and compares them in terms of chemical structure, mode of action and patentability.

Editorial Review

Most newly registered drugs are based on the optimization of existing drugs (natural products, competitive products or in-house lead compounds) with the goal of obtaining an active drug or to diminish side effects. The optimization of known drugs toward certain side effects in itself can open up completely new areas of application.

The editors of the book "Analogue-based Drug Discovery" provide an exact definition of the term analog, and also offer general advice on the available options, but then turn the stage over to experts in the field from industry and research, who illustrate the drug development process in more detail with selected examples in the section "Selected Examples from the Analogue-based Drug Discoveries". With some variability between authors, the chapters are interesting from a historical perspective, pointing out the options for structural optimization, and explaining some of the fascinating medical background. The line-up of drugs includes antibiotics, angiotensin receptor blockers, proton pump inhibitors, calcium antagonists, and many more.

The book is aimed at the advanced reader who already has some fundamental knowledge of medicinal chemistry and is interested in the process of drug development. The reader will encounter chapters that illustrate in detail the important classes of substances that are particularly interesting from the historical, structural and medical perspectives. Some chapters are especially intriguing to read, such as those on the proton pump inhibitors or the quinolone antibiotics, in which the reader learns about the challenges faced by the pharmaceutical industry when developing a marketable drug. Unfortunately, some of the chapters are limited to a brief comparison of drugs within a class, so that the quality of the contributions is quite uneven.

Chapters with an average level of coverage, such as those on the "Development of Opioid Receptor Ligands" or "Development of Organic Nitrates for Coronary Heart Diseases", are still interesting to read; despite their brevity, they contain worthwhile medicinal data and describe a broad array of analogs together with how their properties differ from those of the initial compound.

The reader of this book becomes privy to an enlightened glimpse into the development of interesting drug classes, which makes it very interesting both for advanced students with some fundamental knowledge of medicinal chemistry as well as for professionals working in research and development. Anyone with a penchant for the background and history of important drugs will find this book an enjoyable read.


List of Contributors.
1. Analogues as a Means of Discovering New Drugs.
2. Drug Likeness and Analogue-Based Drug Discovery.
3. Privileged Structures and Analog-Based Drug Discovery.
1. Development of Anti-Ulcer H2-Receptor Histamine Antagonists.
2. Esomeprazole in the Framework of Proton-Pump Inhibitor Development.
3. The Development of a New Proton-Pump Inhibitor: The Case History of Pantoprazole.
4. Optimizing the Clinical Pharmacologic Properties of the HMG-CoA Reductase Inhibitors.
5. Optimizing Antihypertensive Therapy by Angiotensin Receptor Blockers.
6. Optimizing Antihypertensive Therapy by Angiotensin-Converting Enzyme Inhibitors.
7. Case Study of Lacidipine in the Research of New Calcium Antagonists.
8. Selective Beta-Adrenergic Receptor-Blocking Agents.
9. Case Study: "Esmolol Stat".
10. Development of Organic Nitrates for Coronary Heart Disease.
11. Development of Opioid Receptor Ligands.
12. Stigmines.
13. Structural Analogues of Clozapine.
14. Quinolone Antibiotics: The Development of Moxifloxacin.
15. The Development of Bisphosphonates as Drugs.
16. Cisplatin and its Analogs for Cancer Chemotherapy.
17. The History of Drospirenone.
18. Histamine h1 Blockers: From Relative Failures to Blockbusters Within Series of Analogues.
19. Corticosteroids: From Natural Products to Useful Analogues.

An Introduction to Medicinal Chemistry

Graham L. Patrick

Paperback, 776 Pages
4th Edition, 2009
ISBN: 978-0-19-923447-9
Oxford University Press


This lively, highly illustrated text provides undergraduate and postgraduatestudents with an accessible introduction to medicinal chemistry. It covers basicprinciples and background, and then describes the general tactics and strategiesinvolved in developing an effective drug. Through the use of numerous examplesit highlights both the difficulties faced by the medicinal chemist and the greatpotential of rational drug design. The second edition has five new chapters andis updated to include recent advances in the field.

Editoral Review

soon available


1 Drugs and the medicinal chemist
2 The why and the wherefore
3 Protein structure
4 Drug action at enzymes
5 Drug action at receptors
6 Receptor
7 Nucleic acids
8 Drug discovery and drug development
9 Drug design - drug/target interactions
10 Pharmacokinetics
11 Quantitative structure-activity relationships (QSAR)
12 Combinatorial synthesis
13 Computers in medicinal chemistry
14 Antibacterial agents
15 The peripheral nervous system-cholinergics, anticholinergics, andanticholinesterases
16 The adrenergic nervous system
17 The opium analgesics
18 Cimetidine - a rational approach to drug design
Further reading

Chirality in Drug Research

Eric Francotte, Wolfgang Lindner

Hardcover, 351 Pages
First Edition, 2006
ISBN: 3-527-31076-2


Divided into the three main sections of synthesis, analysis and drug development, this handbook covers all stages of the drug development process, including large-scale synthesis and purification of chirally pure pharmaceuticals.

The two editors from academia and a major pharmaceutical company have assembled an experienced, international team who provide first-hand practical advice and report previously unpublished data.

In the first section, the isolation of chiral drugs from natural sources, their production in enzymatic processes and the resolution of racemic mixtures in preparative chromatography are outlined in separate chapters. For the section on qualitative and quantitative analysis, enantioselective chromatographic methods are presented as well as optical methods and CE-MS, while the final section deals with the pharmacology, pharmacokinetics and metabolic aspects of chiral drugs, devoting whole chapters to stereoselective drug binding and modeling chiral drug-receptor interactions.

With its unique industry-relevant aspects, this is a must for medicinal and pharmaceutical chemists.

Editorial Review

One reason behind the trend for medications to contain an active drug in the most enantiomerically enriched form possible is the availability of better methods for enantioselective synthesis and characterization. However, a greater knowledge of the biology involved is far more significant, as exemplified in particular by the tragic thalidomide episode, and this has led to paradigm shifts both in the industry and on approval boards. The other enantiomer frequently amounts only to so much inactive dead weight, while a number of such enantiomers are responsible for side effects; only in a few cases have specific compositions of a racemate or an enantiomeric pair demonstrated a synergistic effect.

During the actual development process, the question invariably arises of which step and which method to choose for introducing enrichment. Thus racemates are produced by parallel synthesis for drug candidates - it makes sense to resolve the racemate for the initial animal studies, whereas an optimized, enantioselective synthesis is employed in the course of production. These steps go hand in hand, so that the initial experiences in optimization (method development for analysis, and for synthesis and purification) are transferred directly into the next stage of development.

The book “Chirality in Drug Research” explains in detail why enantiomers should be considered as completely different drugs as a matter of principle, and provides a good and easily understood survey of the most important methods used in industry for the manufacture and analysis of drugs. It is indeed difficult for a single book to cover all of the different stages of development, all the way from the milligram-scale up to tonnes, but the present work appears to have succeeded in this regard. This monograph is ideal in that it provides an overview of the methods and technologies currently in use, and refers the reader to cited literature for more in-depth study where necessary. It can facilitate collaborations between the individual work groups involved in development, since all of the important principles and options are introduced. This work’s interdisciplinary character is also a boon for advanced students, making it an interesting read for those who wish to gain a greater familiarity with this area. “Chirality in Drug Research” provides its readers with a comprehensive overview of the field, and offers a simultaneous, integrated exposure to the important methods for both synthesis and analysis.


1 Chiral Drugs from a Historical Point of View (Joseph Gal).
2 Stereoselective Synthesis of Drugs – An Industrial Perspective (Hans-Jürgen Federsel).
3 Aspects of Chirality in Natural Products Drug Discovery (Philipp Krastel, Frank Petersen, Silvio Roggo, Esther Schmitt, and Ansgar Schuffenhauer).
4 Biotransformation Methods for Preparing Chiral Drugs and Drug Intermediates (Michael Müller and Marcel Wubbolts).
5 Resolution of Chiral Drugs and Drug Intermediates by Crystallisation (Kazuhiko Saigo).
6 Isolation and Production of Optically Pure Drugs by Enantioselective Chromatography (Eric Francotte).
7 Stereoselective Chromatographic Methods for Drug Analysis (Norbert M. Maier and Wolfgang Lindner).
8 Capillary Electrophoresis Coupled to Mass Spectrometry for Chiral Drugs Analysis (Serge Rudaz and Jean-Luc Veuthey).
9 Powerful Chiral Molecular Tools for Preparation of Enantiopure Alcohols and Simultaneous Determination of Their Absolute Configurations by X-Ray Crystallography and/or 1H NMR Anisotropy Methods (Nobuyuki Harada).
10 Keywords in Chirality Modeling Molecular Modeling of Chirality – Software and Literature Research on Chirality in Modeling, Chirality in Docking, Chiral Ligand–Receptor Interaction and Symmetry (Gerd Folkers, Mine Yarim, and Pavel Pospisil).

Contemporary Drug Synthesis

Jie Jack Li, Douglas S. Johnson, Drago R. Sliskovic, Bruce D. Roth

Hardcover, 221Pages

FirstEdition, June 2004
ISBN: 0-471-21480-9


An integrated and insightful look at successful drug synthesis in today’sdrug discovery market
The pharmaceutical industry is unquestionably vibrant today, with drug synthesismaking a vital contribution. Whether in the early developmental stages ofidentifying and optimizing a lead, or the latter stages of process developmentand cost-effective scale-up, the ability to design elegant and economicalsynthetic routes is often a major factor in the eventual viability andcommercial success of a drug.

Contemporary Drug Synthesis examines how leading researchers and manufacturershave integrated chemistry, biology, pharmacokinetics, and a host of otherdisciplines in the creation and development of leading drugs. Authored by fourof the pharmaceutical industry’s most respected scientists, this timely volume:

  • Focuses on the processes that resulted in high-profile drugs includingLipitor, Celebrex, Viagra, Gleevec, Nexium, Claritin, and over a dozenothers
  • Provides an in-depth introduction to each drug, followed by a detailedaccount of its synthesis 
  • Organizes the drugs into fourteen therapeutic areas for clarity and easeof use

Process chemists provide an essential bridge between chemistry and themarketplace, creating scientifically practical drug processes while never losingsight of the commercial viability of those processes. Contemporary DrugSynthesis meets the needs of a growing community of researchers inpharmaceutical research and development, and is both a useful guide forpracticing pharmaceutical scientists and an excellent text for medicinal andorganic chemistry students.

Editorial Review

"Contemporary Drug Synthesis" is a highly interesting book thatillustrates the syntheses of a number of important drugs. A briefpresentation of the associated biological background material isprovided for the individual of compound classes, but the syntheticpathways take center stage. When several different pathways aredescribed, the author enumerates the pros and cons of each.

It is noteworthy that the book keeps to the facts, and the emphasis is onan all-inclusive treatment of the extant and significant pathways. Whileit is true that the number of drugs discussed is limited, the impressionis that the most interesting ones have been selected. The reader doesneed a fairly advanced prior knowledge of organic chemistry in order toderive the most benefit from these readings. "Contemporary DrugSynthesis" doesn't take the place of a textbook, since the comparisonsbetween the different methods and pathways are rather too brief for thispurpose.

This work is intended for anyone who is interested in the synthesis ofdrugs. For students who anticipate specializing in this field, inaddition to the traditional medicinal chemistry textbook that providesthem with more on the underlying biochemistry, it is recommended thatthey have a look at this book as well. Even experienced medicinalchemists who consult this work will find themselves inspired with newapproaches.


Chapter 1. Antithrombotics: Ticlopidine (Ticlid®) and Clopidogrel (Plavix®).
Chapter 2. Anti-inflammatory Cyclooxygenase-2 Selective Inhibitors: Celecoxib(Celebrex®) and Rofecoxib (Vioxx®).
Chapter 3. H+/K+ -ATPase Inhibitors: Esomeprazole (Nexium®).
Chapter 4. Protein-tyrosine Kinase Inhibitors: Imatnib (Gleevec®) and Gefitinib(Iressa®).
Chapter 5. Non-sedating Antihistamines.
Chapter 6. Cosmeceuticals: Istretinoin (Accutane®), Tazarotene (Tazorac®),Minoxidil (Rogaine®), and Finasteride (Propecia®).
Chapter 7. Antibacterials: Ciprofloxacin (Cipro®) and Linezolid (Zyvox®).
Chapter 8. Atypical Antupsychotics.
Chapter 9. Atovastatin Calcium (Lipitor®).
Chapter 10. Antidepressants.
Chapter 11. Anti-obesity: Orlistat (Xenical®).
Chapter 12. Triptans for Migrane.
Chapter 13. PDE 5 Inhibitors for Erectile Dysfunction: Sildenafil (Viagra®),Vardenafil (Levitra®), and Tadalafil (Cialis®).
Chapter 14. Antiasthmatics.

Fundamentals of Medicinal Chemistry

Gareth Thomas

Paperback, 285 Pages
First Edition, December 2003
ISBN: 0-470-84307-1
John Wiley & Sons Inc


Provides a concise introduction to the chemistry of therapeutically activecompounds, written in a readable and accessible style.
The title begins by reviewing the structures and nomenclature of the morecommon classes of naturally occurring compounds found in biological organisms.An overview of medicinal chemistry is followed by chapters covering thediscovery and design of drugs, pharmacokinetics and drug metabolism, The bookconcludes with a chapter on organic synthesis, followed by a brief look at drugdevelopment from the research stage through to marketing the final product.

The text assumes little in the way of prior biological knowledge. relevantbiology is included through biological topics, examples and the Appendices.

Incorporates summary sections, examples, applications and problems
Each chapter contains an additional summary section and solutions to thequestions are provided at the end of the text
Invaluable for undergraduates studying within the chemical, pharmaceuticaland life sciences.

Editorial Review

soon available.


1. Biological Molecules.
2. An Introduction to Drugs and Their Action.
3. An Introduction to Drug Discovery.
4. The SAR and QSAR Approaches to Drug Design.
5. Computer Aided Drug Design.
6. Combinatorial Chemistry.
7. Selected Examples of Drug Action at some Common Target Areas.
8. Pharmacokinetics.
9. Drug Metabolism.
10. An Introduction to Lead and Analogue Syntheses.
11. Drug Development and Production.
Appendix 1. Sickle-cell Anaemia.
Appendix 2. Bacteria.
Appendix 3. Cell Membranes.
Appendix 4. Receptors.
Appendix 5. Transfer through Membranes.
Appendix 6. Regression Analysis.
Appendix 7. Enzymes.
Answers to Questions.
Selected Further Reading.

Index Nominum: International Drug Directory


Hardcover, 2889 Pages
20th Edition, 2011
ISBN: 978-3-8047-5053-1


Are you looking for a German pharmaceutical preparation that is not longer on the market? Or an equivalent preparation available in another country? Are you faced with a prescription for a foreign preparation? No problem!
This unique pharmaceutical index includes

  • 5100 active substances (and derivatives) with international non-proprietary names (INN), German, French, Spanish and Latin substance names, structural and molecular formulas, CAS registry numbers and 15,500 synonyms,
  • 70,000 proprietary names from more than 16,500 manufacturers from 171 countries,
  • therapeutic groups with ATC codes of the WHO for pharmaceuticals used in human and veterinary medicine,
  • valuable search assistance with an alphabetical index of all trade names, pharmaceutical substances and synonyms as well as a separate ATC and ATCvet substance index.

Editorial Review

For more than 50 years, Index Nominum has been the definitive work for the names of brand-name drugs, through which the structures and CAS Reg. Nos. of the corresponding active ingredients can readily be found. The detailed index of brand names can, for example, provide the pharmacist who is faced with a foreign prescription with a list of the corresponding domestic drug products. On the other hand, the listing (on a CD-ROM) of the names and addresses of the manufacturers of the respective drugs is of interest for purposes of cooperation between pharmaceutical companies.

The Index Nominum covers a seemingly endless number of commercial names and manufacturing companies, which are arranged according to the actual drug substance. Despite the information from the chemical perspective being limited to the structure and chemical synonyms (CAS Reg No, CAS name, IUPAC name), and the drug action being described merely in one or two words (e.g., “antidepressant”), doing a commercial name search in the Index Nominum facilitates entry into the broader literature.

It is a pity that the CD-ROM gives only the addresses of the manufacturing companies, and that there is no structurally searchable form of the Index Nominum. Structure-searchable databases on the internet are more interesting to chemists, but for the most part these so far do not contain a treasure trove of specialized information: the multitude of names from the Index Nominum. The Index Nominum is really not needed on a daily basis in research; it serves its purpose instead as a library resource. However, a personal copy is definitely recommended for pharmacists and medical doctors..

Lehninger Principles of Biochemistry

David L. Nelson, Michael M. Cox

Hardcover, 1100 Pages
5th Edition, 2008
ISBN: 978-0-716-77108-1
Palgrave Macmillan


In the Fifth Edition, authors Dave Nelson and Mike Cox combine the best of the laboratory and best of the classroom, introducing exciting new developments while communicating basic principles through a variety of new learning tools such as new in-text worked examples and data analysis problems.

Editorial Review

Lehninger’s Principles of Biochemistry is a very comprehensive book, in which a surprising number of current subjects that reflect the state of the art are described with unique illustrations. The reader must have some basic chemical knowledge to understand the text, and in some places the authors refer back to subjects that are only discussed in detail later on. In any case, the work overall is readily understandable, and is elaborately detailed for use both for learning and as a reference.

Thus, with illustrations that are of top-level quality and content that is kept simple and readable, these two work very well together. This is definitely not a case of pretty pictures being used to obscure weaknesses in the wording! Readers who are still obliged to learn from older biochemistry textbooks should take a look at Lehninger in this regard, since the authors have succeeded in exemplifying the newest methods and findings with truly well-crafted diagrams and text. It is well known that, thanks to structure elucidation, the spatial arrangement of biomolecules and the resulting effects on their function have become a focus of attention in science. These rapid advances are covered definitively in Lehninger.

On all accounts, the many modifications between the 4th and 5th edition bring the book into line with the latest research. The scope of this work also warrants its purchase, since one can be almost certain just from the Table of Contents that Lehninger has the important areas covered. Though some students will probably be taken aback at the shear wealth of information, they nevertheless will have a book that proves quite handy later in their careers, when they need to find the details of the biochemical principles that underlie specific problems. Lehninger is also recommended for those who are already working in medicinal chemistry or related areas, since in addition to the elementary background material contained, current research topics such as signal transduction are addressed in exacting detail in the book. In many subject areas, Lehninger even bridges the gap to modern drug discovery, since a number of drugs and their functions are described in information boxes scattered throughout the text.

"Principles of Biochemistry" will be interesting to anyone who plans to work in the life sciences industry. Lehninger is a good tool for those students who intend to specialize in molecular biology, although the coverage is apt to be too comprehensive for others. The book is nevertheless a worthwhile investment, since one finds therein practically all the topics in biochemistry, each with detailed and well-illustrated explanations.


1 The Foundations of Biochemistry
1.1 Cellular Foundations
1.2 Chemical Foundations
1.3 Physical Foundations
1.4 Genetic Foundations
1.5 Evolutionary Foundations
Box 1–1 Molecular Weight, Molecular Mass, and Their Correct Units
Box 1–2 Louis Pasteur and Optical Activity: In Vino, Veritas
Box 1–3 Entropy: The Advantages of Being Disorganized
• Now introduces the concepts of proteomes and proteomics
• Updated section on how a new species evolves
• Increased emphasis on the interdependence of life forms in global cycles of energy

2 Water
2.1 Weak Interactions in Aqueous Systems
2.2 Ionization of Water, Weak Acids, and Weak Bases
2.3 Buffering against pH Changes in Biological Systems
2.4 Water as a Reactant
2.5 The Fitness of the Aqueous Environment for Living Organisms
Box 2–1 Medicine: On Being One’s Own Rabbit (Don’t Try This at Home!)
• Expanded discussion of blood pH buffering by the bicarbonate system,including a new box describing Haldane’s use of himself as a guinea pig    in experiments aimed at changing the acidity of blood
• New section on ketoacidosis in diabetes

3 Amino Acids, Peptides, and Proteins
3.1 Amino Acids
3.2 Peptides and Proteins
3.3 Working with Proteins
3.4 The Structure of Proteins: Primary Structure
Box 3–1 Methods: Absorption of Light by Molecules: The Lambert-Beer Law
Box 3–2 Methods: Investigating Proteins with Mass Spectrometry
Box 3–3 Medicine: Consensus Sequences and Sequence Logos
• Significant revision to bioinformatics
• More thorough explanation of consensus sequences, including an illustration of common ways to depict consensus sequences

4 The Three-Dimensional Structure of Proteins
4.1 Overview of Protein Structure
4.2 Protein Secondary Structure
4.3 Protein Tertiary and Quaternary Structures
4.4 Protein Denaturation and Folding
Box 4–1 Methods: Knowing the Right Hand from the Left
Box 4–2 Permanent Waving Is Biochemical Engineering
Box 4–3 Medicine: Why Sailors, Explorers, and College Students Should  Eat Their Fresh Fruits and Vegetables
Box 4–4 The Protein Data Bank
Box 4–5 Methods: Methods for Determining the Three-Dimensional Structure of a Protein
Box 4–6 Medicine: Death by Misfolding: The Prion Diseases
• New section, Defects in protein folding may be the molecular basis for a wide range of human genetic disorders, discusses a variety of amyloid    diseases
• New section on circular dichroism

5 Protein Function
5.1 Reversible Binding of a Protein to a Ligand: Oxygen-Binding Proteins
5.2 Complementary Interactions between Proteins and Ligands: The Immune System and Immunoglobulins
5.3 Protein Interactions Modulated by Chemical Energy: Actin, Myosin, and Molecular Motors
Box 5–1 Medicine: Carbon Monoxide: A Stealthy Killer

6 Enzymes
6.1 An Introduction to Enzymes
6.2 How Enzymes Work
6.3 Enzyme Kinetics as an Approach to Understanding Mechanism
6.4 Examples of Enzymatic Reactions
6.5 Regulatory Enzymes
Box 6–1 Transformations of the Michaelis-Menten Equation: The Double-Reciprocal Plot
Box 6–2 Kinetic Tests for Determining Inhibition Mechanisms
Box 6–3 Evidence for Enzyme–Transition State Complementarity
• More explanatory text added to the mechanisms for the enolase and lysozyme reactions
• New section on pharmaceuticals developed from an understanding of enzyme mechanism, using penicillin and HIV protease inhibitors as examples

7 Carbohydrates and Glycobiology
7.1 Monosaccharides and Disaccharides
7.2 Polysaccharides
7.3 Glycoconjugates: Proteoglycans, Glycoproteins, and Glycolipids
7.4 Carbohydrates as Informational Molecules: The Sugar Code
7.5 Working with Carbohydrates
Box 7–1 Medicine: Blood Glucose Measurements in the Diagnosis and Treatment of Diabetes
• New medical box, introduces hemoglobin glycation and AGEs and their role in the pathology of advanced diabetes
• New section on sugar analogs as drugs that target viral neuraminidase
• Introduction to the new field of glycomics, including methods for determining oligosaccharide structure using MALDI-MS

8 Nucleotides and Nucleic Acids
8.1 Some Basics
8.2 Nucleic Acid Structure
8.3 Nucleic Acid Chemistry
8.4 Other Functions of Nucleotides

9 DNA-Based Information Technologies
9.1 DNA Cloning: The Basics
9.2 From Genes to Genomes
9.3 From Genomes to Proteomes
9.4 Genome Alterations and New Products of Biotechnology
Box 9–1 Medicine: A Potent Weapon in Forensic Medicine
Box 9–2 Medicine: The Human Genome and Human Gene Therapy
• New material on the green fluorescent protein
• Thorough updating of genomics section

10 Lipids
10.1 Storage Lipids
10.2 Structural Lipids in Membranes
10.3 Lipids as Signals, Cofactors, and Pigments
10.4 Working with Lipids
Box 10–1 Sperm Whales: Fatheads of the Deep
Box 10–2 Medicine: Abnormal Accumulations of Membrane Lipids: Some Inherited Human Diseases
• New medical section on the role of polyunsaturated fatty acids and trans fatty acids in cardiovascular disease
• New section on lipidomics
• New descriptions of volatile lipids used as signals by plants, and pigments of bird feathers derived from colored lipids in plant foods

11 Biological Membranes and Transport
11.1 The Composition and Architecture of Membranes
11.2 Membrane Dynamics
11.3 Solute Transport across Membranes
Box 11–1 Methods: Atomic Force Microscopy to Visualize Membrane Proteins
Box 11–2 Medicine: Defective Glucose and Water Transport in Two Forms of Diabetes
Box 11–3 Medicine: A Defective Ion Channel in Cystic Fibrosis
• Expanded section on bilayer dynamics covers flippases, floppases, scramblases, and bilayer asymmetry
• Expanded and updated section on lipid rafts and caveolae includes new  material on membrane curvature and the proteins that influence it, and    introduces amphitropic proteins and annular lipids
• New information on the structural basis for voltage gating in a K+ channel

12 Biosignaling
12.1 General Features of Signal Transduction
12.2 G Protein–Coupled Receptors and Second Messengers
12.3 Receptor Tyrosine Kinases
12.4 Receptor Guanylyl Cyclases, cGMP, and Protein Kinase G
12.5 Multivalent Scaffold Proteins and Membrane Rafts
12.6 Gated Ion Channels
12.7 Integrins: Bidirectional Cell Adhesion Receptors
12.8 Regulation of Transcription by Steroid Hormones
12.9 Signaling in Microorganisms and Plants
12.10 Sensory Transduction in Vision, Olfaction, and Gustation
12.11 Regulation of the Cell Cycle by Protein Kinases
12.12 Oncogenes, Tumor Suppressor Genes, and Programmed Cell Death
Box 12–1 Methods: Scatchard Analysis Quantifies the Receptor-Ligand Interaction
Box 12–2 Medicine: G Proteins: Binary Switches in Health and Disease
Box 12–3 Methods: FRET: Biochemistry Visualized in a Living Cell
Box 12–4 Medicine: Color Blindness: John Dalton’s Experiment from the Grave
Box 12–5 Medicine: Development of Protein Kinase Inhibitors for Cancer Treatment
• New Medical section on G protein coupled receptors (GCPRs) discusses the range of diseases for which drugs target GPCRs
• New box on G proteins, proteins that regulate their GTPase activity, and the medical consequences of defective G protein function
• Expanded and integrated treatment of local signaling circuits, including AKAPs and signaling complexes that include protein kinase   A, adenylyl cyclase, and phosphodiesterase, and localized puffs and    waves of Ca2+
• New medical box on the use of protein kinase inhibitors in cancertherapy

13 Bioenergetics and Biochemical Reaction Types
13.1 Bioenergetics and Thermodynamics
13.2 Chemical Logic and Common Biochemical Reactions
13.3 Phosphoryl Group Transfers and ATP
13.4 Biological Oxidation-Reduction Reactions
Box 13–1 Firefly Flashes: Glowing Reports of ATP
• New section, Chemical logic and common biochemical reactions, discusses common biochemical reaction types

14 Glycolysis, Gluconeogenesis, and the Pentose Phosphate Pathway
14.1 Glycolysis
14.2 Feeder Pathways for Glycolysis
14.3 Fates of Pyruvate under Anaerobic Conditions: Fermentation
14.4 Gluconeogenesis
14.5 Pentose Phosphate Pathway of Glucose Oxidation
Box 14–1 Medicine: High Rate of Glycolysis in Tumors Suggests Targets for Chemotherapy and Facilitates Diagnosis
Box 14–2 Athletes, Alligators, and Coelacanths: Glycolysis at Limiting Concentrations of Oxygen
Box 14–3 Ethanol Fermentations: Brewing Beer and Producing Biofuels
Box 14–4 Medicine: Why Pythagoras Wouldn’t Eat Falafel: Glucose 6-Phosphate Dehydrogenase Deficiency
• New medical box on glucose uptake deficiency in type 1 diabetes
• New medical box on how the high rate of glycolysis in cancerous tissue aids cancer diagnosis and treatment

15 Principles of Metabolic Regulation
15.1 Regulation of Metabolic Pathways
15.2 Analysis of Metabolic Control
15.3 Coordinated Regulation of Glycolysis and Gluconeogenesis
15.4 The Metabolism of Glycogen in Animals
15.5 Coordinated Regulation of Glycogen Synthesis and Breakdown
Box 15–1 Methods: Metabolic Control Analysis: Quantitative Aspects
Box 15–2 Isozymes: Different Proteins That Catalyze the Same Reaction
Box 15–3 Medicine: Genetic Mutations That Lead to Rare Forms of Diabetes
Box 15–4 Carl and Gerty Cori: Pioneers in Glycogen Metabolism and Disease
• New section on emerging role of ribulose 5-phosphate as central regulator of glycolysis and gluconeogenesis
• Expanded discussion of phosphoprotein phosphatases in metabolic regulation
• Expanded coverage of the role of transcriptional regulators in metabolic regulation
• New medical box on mutations that lead to rare forms of diabetes regulation (MODY)

16 The Citric Acid Cycle
16.1 Production of Acetyl-CoA (Activated Acetate)
16.2 Reactions of the Citric Acid Cycle
16.3 Regulation of the Citric Acid Cycle
16.4 The Glyoxylate Cycle
Box 16–1 Moonlighting Enzymes: Proteins with More Than One Job
Box 16–2 Synthases and Synthetases; Ligases and Lyases; Kinases,Phosphatases, and Phosphorylases: Yes, the Names Are Confusing!
Box 16–3 Citrate: A Symmetric Molecule That Reacts Asymmetrically
Box 16–4 Citrate Synthase, Soda Pop, and the World Food Supply
• New box on effect of diabetes on the citric acid cycle and ketone body formation
• Expanded discussion of substrate channeling
• New section on mutations in citric acid cycle that lead to cancer
• New box on moonlighting enzymes

17 Fatty Acid Catabolism
17.1 Digestion, Mobilization, and Transport of Fats
17.2 Oxidation of Fatty Acids
17.3 Ketone Bodies
Box 17–1 Fat Bears Carry Out b Oxidation in Their Sleep
Box 17–2 Coenzyme B12: A Radical Solution to a Perplexing Problem
• New section on the role of transcription factors (PPARs) in regulation of lipid catabolism

18 Amino Acid Oxidation and the Production of Urea
18.1 Metabolic Fates of Amino Groups
18.2 Nitrogen Excretion and the Urea Cycle
18.3 Pathways of Amino Acid Degradation
Box 18–1 Medicine: Assays for Tissue Damage
Box 18–2 Medicine: Scientific Sleuths Solve a Murder Mystery
• New section on pernicious anemia and associated problems in strict vegetarians.

19 Oxidative Phosphorylation and Photophosphorylation
Oxidative Phosphorylation

19.1 Electron-Transfer Reactions in Mitochondria
19.2 ATP Synthesis
19.3 Regulation of Oxidative Phosphorylation
19.4 Mitochondria in Thermogenesis, Steroid Synthesis, and Apoptosis
19.5 Mitochondrial Genes: Their Origin and the Effects of Mutations

Photosynthesis: Harvesting Light Energy
19.6 General Features of Photophosphorylation
19.7 Light Absorption
19.8 The Central Photochemical Event: Light-Driven Electron Flow
19.9 ATP Synthesis by Photophosphorylation
19.10 The Evolution of Oxygenic Photosynthesis
Box 19–1 Hot, Stinking Plants and Alternative Respiratory Pathways
• Updated discussion of the structure of the electron transfer complexes of mitochondria and chloroplasts, and of the Fo complex
• Updated description of the water-splitting complex’s structure in chloroplasts
• Expanded description of mitochondrial diseases and mitochondrial role in diabetes

20 Carbohydrate Biosynthesis in Plants and Bacteria
20.1 Photosynthetic Carbohydrate Synthesis
20.2 Photorespiration and the C4 and CAM Pathways
20.3 Biosynthesis of Starch and Sucrose
20.4 Synthesis of Cell Wall Polysaccharides: Plant Cellulose and Bacterial Peptidoglycan
20.5 Integration of Carbohydrate Metabolism in the Plant Cell

21 Lipid Biosynthesis
21.1 Biosynthesis of Fatty Acids and Eicosanoids
21.2 Biosynthesis of Triacylglycerols
21.3 Biosynthesis of Membrane Phospholipids
21.4 Biosynthesis of Cholesterol, Steroids, and Isoprenoids
Box 21–1 Mixed-Function Oxidases, Oxygenases, and Cytochrome P-450
• Revised and updated section on fatty acid synthase includes new structural information on FAS I
• Updated information on cyclooxygenase inhibitors (pain relievers Vioxx, Celebrex, Bextra)
• New information on HMG-CoA reductase and new medical box on statins

22 Biosynthesis of Amino Acids, Nucleotides, and Related Molecules
22.1 Overview of Nitrogen Metabolism
22.2 Biosynthesis of Amino Acids
22.3 Molecules Derived from Amino Acids
22.4 Biosynthesis and Degradation of Nucleotides
Box 22–1 Unusual lifestyles of the obscure but abundant
Box 22–2 Medicine: On Kings and Vampires
Box 22–3 Medicine: Curing African Sleeping Sickness with a Biochemical Trojan Horse
• Updated coverage of nitrogen cycle section includes a new box on anammox bacteria
• New information on therapy for acute lymphoblastic leukemia
• New information on folic acid deficiency

23 Hormonal Regulation and Integration of Mammalian Metabolism
23.1 Hormones: Diverse Structures for Diverse Functions
23.2 Tissue-Specific Metabolism: The Division of Labor
23.3 Hormonal Regulation of Fuel Metabolism
23.4 Obesity and the Regulation of Body Mass
23.5 Obesity, the Metabolic Syndrome, and Type 2 Diabetes
Box 23–1 Medicine: How Is a Hormone Discovered? The Arduous Path to Purified Insulin
• Expanded coverage and updating of the biochemical connections between obesity, metabolic syndrome, and type 2 diabetes
• Updated discussion of the integration of fuel metabolism in fed and starved states in diabetes

24 Genes and Chromosomes
24.1 Chromosomal Elements
24.2 DNA Supercoiling
24.3 The Structure of Chromosomes
Box 24–1 Medicine: Curing Disease by Inhibiting Topoisomerases
Box 24–2 Medicine: Epigenetics, Nucleosome Structure, and Histone Variants
• New material on histone modification, histone variants, and nucleosome deposition
• New medical box on the use of topoisomerase inhibitors in the treatment of bacterial infections and cancer, includes material on ciprofloxacin (the    antibiotic effective for anthrax)
• New box on the role of histone modification and nucleosome deposition in the transmission of epigenetic information in heredity

25 DNA Metabolism
25.1 DNA Replication
25.2 DNA Repair
25.3 DNA Recombination
Box 25–1 Medicine: DNA Repair and Cancer
• New information on the initiation of replication and the dynamics at the replication fork, introducing AAA+ ATPases and their functions in replication and other aspects of DNA metabolism

26 RNA Metabolism
26.1 DNA-Dependent Synthesis of RNA
26.2 RNA Processing
26.3 RNA-Dependent Synthesis of RNA and DNA
Box 26–1 Methods: RNA Polymerase Leaves Its Footprint on a Promoter
Box 26–2 Fighting AIDS with Inhibitors of HIV Reverse Transcriptase
Box 26–3 Methods: The SELEX Method for Generating RNA Polymers with New Functions
Box 26–4 An Expanding RNA Universe Filled with TUF RNAs
• New section on the expanding roles of RNA in cells

27 Protein Metabolism
27.1 The Genetic Code
27.2 Protein Synthesis
27.3 Protein Targeting and Degradation
Box 27–1 Exceptions That Prove the Rule: Natural Variations in the Genetic Code
Box 27–2 From an RNA World to a Protein World
Box 27–3 Natural and Unnatural Expansion of the Genetic Code
Box 27–4 Induced Variation in the Genetic Code: Nonsense Suppression
• Expanded section on protein synthesis coupled to the advances in ribosome structure
• New information on the roles of RNA in protein biosynthesis

28 Regulation of Gene Expression
28.1 Principles of Gene Regulation
28.2 Regulation of Gene Expression in Bacteria
28.3 Regulation of Gene Expression in Eukaryotes
Box 28–1 Of Fins, Wings, Beaks, and Things
• New information about roles of RNA in gene regulation
• New box on the connections between evolution and development

Molecules and Medicine

E. J. Corey, László Kürti, Barbara Czakó

Softcover, 272 Pages
First Edition, 2007
ISBN: 978-0-470-22749-7


Molecules and Medicine provides, for the first time ever, a completely integrated look at chemistry, biology, drug discovery, and medicine. Beautifully illustrated and presented in full colour, this book delves into the discovery, application, and mode of action of more than one hundred of the most significant molecules now used in modern medicine.

With focus on the most important and commonly used medicines such as anti-clotting agents, antibiotics, Viagra and anti-malarial and antidepressant drugs, coverage includes the condition it treats, the summary of its industrial development, the year put into practice, the biological target for the medicine, the human proteins related to the disease, the metabolism or action of the condition treated, and interacting side effects and related drugs. Diagrams revealing the shape and structure of molecular make-up for each medicine accompany the text. Interspersed where appropriate, can be found background sections such as a brief survey of immunology, to help guide the readers understanding.

Editorial Review

Molecules and Medicine is directed at a broad audience, and tries to explain drugs and diseases in an understandable way. Thus, the book even contains an introduction on the make-up of molecules, where the fundamentals of structure and bonding are explained. This introduction is nicely done and contains attractive pictures, but students will know these principles from other books, and I doubt if a reader without any chemical training will be able to follow them at the pace they are presented. This chapter is much too short, and the concepts of medicinal chemistry are not mentioned. Thus, the reader will miss out on understanding the biochemical principles and important molecular properties that are responsible for the intermolecular interactions with a target; these latter are far more conducive to an understanding of drug development than isolated observations on orbitals and three-dimensional biological macromolecules. The untrained reader might have more interest in the various stages of drug development, but will find nothing about this in the book, and so will never appreciate the efforts and costs that must be expended for each of the drugs described in the following chapters to reach commercialization.

However, readers who have the benefit of chemical, biochemical and medicinal chemical training from the corresponding textbooks should certainly take a look at this book, since the subsequent chapters are recommendable on the strength of their brief and readable illustrations of the important targets and drugs. The biochemistry behind specific diseases is explained schematically, drugs are displayed as structures and 3D models, and for some molecules a depiction of the inhibited enzyme is also provided. Here, the reader will find citations to supplemental literature on interesting diseases, introductory explanations and a multitude of commercial drugs; on this basis, the book can be recommended to obtain a general overview of current research trends as well as an introduction to a specific topic.


Acetylsalicylic acid (Aspirin™)
Naproxen (Aleve™)
How Do Anti-Inflammatory Drugs Work?.
Other Eicosanoids in Inflammation
An Overview of Inflammation
Celecoxib (Celebrex™).
Prednisone (Deltasone™)
Methotrexate (Trexall™)
Allopurinol (Zyloprim™)
Salmeterol (Advair™)
Fluticasone Propionate (Flovent™).
Montelukast Sodium (Singulair™).Tiotropium Bromide (Spiriva™).
Loratadine (Claritin™)
An Overview of Metabolic Syndrome
Metformin (Glucophage™)
Glipizide (Glucotrol™)
Pioglitazone (Actos™)
Sitagliptin (Januvia™)
Atorvastatin (Lipitor™)
Ezetimibe (Zetia™)
Atenolol (Tenormin™)
Enalapril (Vasotec™)
Candesartan Ciletexil (Atacand™)
Aliskiren (Tekturna™)
Amlodipine (Norvasc™)
Clopidogrel Bisulfate (Plavix™)
Digoxin (Lanoxin™)
Information Flow into the Cell by Chemical Signaling.
Oral Contraceptives
Mifepristone (Mifeprex™)
Oxytocin (Oxytocin™)
Sildenafil (Viagra™)
Some Aspects of Osteoporosis
Alendronate (Fosamax™).
Calcitriol (Rocaltrol™)
Raloxifene (Evista™)
Teriparatide (Forteo™)
Latanoprost (Xalatan™)
Ranitidine (Zantac™)
Omeprazole (Prilosec™)
A Brief Survey of the Immune System
Azathioprine (Imuran™)
Mycophenolate Mofetil (CellCept™)
Cyclosporin (Neoral™)
Tacrolimus (Prograf™)
FTY720 (Fingolimod)
Amoxicillin (Amoxil™)
Cefaclor (Ceclor™)
Doxycycline (Vibramycin™)
Azithromycin (Zithromax™)
Ciprofloxacin (Cipro™)
Trimethoprim (Triprim™)
Amikacin (Amikin™)
Vancomycin (Vancocin™)
Linezolid (Zyvox™)
Isoniazid (Laniazid™)
Ancillary Antibiotics
Drug Resistance
On Viruses and Viral Diseases
Acyclovir (Zovirax™)
Ribavirin (Virazole™)
Oseltamivir (Tamiflu™)
Zidovudine (Retrovir, AZT™)
Zalcitabine (Hivid™)
Nevirapine (Viramune™)
Efavirenz (Sustiva™)
Lopinavir + Ritonavir (Kaletra™)
UK427857 (Maraviroc)
Amphotericin (Fungilin™)
Fluconazole (Diflucan™)
Caspofungin (Cancidas™)
Terbinafine (Lamisil™)
Parasitic Diseases: A Focus on Malaria
Chloroquine (Aralen™)
Artemether + Lumefantrine (CoArtem™)
Atovaquone + Proguanil (Malarone™)
Miltefosine (Impavido™)
Nitazoxanide (Alinia™)
Ivermectin (Stromectol™)
An Overview of Cancer
Capecitabine (Xeloda™)
Carboplatin (Paraplatin™)
Vinblastine (Velban™)
Paclitaxel (Taxol™)
Cyclophosphamide (Cytoxan™)
Tamoxifen (Nolvadex™)
Irinotecan (Camptosar™)
Bleomycin (Blenoxane™)
Imatinib (Gleevec™)
Sunitinib (Sutent™)
Bortezomib (Velcade™)
Ancillary Anticancer Agents
Lidocaine (Xylocaine™)
Morphine (Avinza™)
Acetaminophen (Tylenol™)
Fentanyl (Duragesic™)
Sodium Thiopental (Sodium Pentothal™)
Gabapentin (Neurontin™)
Diazepam (Valium™)
Sumatriptan (Imitrex™)
Zolpidem (Ambien™)
Ramelteon (Rozerem™)
Varenicline (Chantix™)
The Brain, Neurotransmission and Neurotransmitters
Levodopa (Larodopa™)
Donepezil (Aricept™)

Pharmaceutical Substances

A. Kleemann, J. Engel, B. Kutscher, D. Reichert

Hardcover,2286 Pages
4th Edition,2001
ISBN: 3-13558-404-6
Georg Thieme Verlag


The 4th edition of Pharmaceutical Substances isdesigned to be a complete reference guide to every pharmaceuticalcompound of significance. It provides a compendium of nearly 2300pharmaceutical ingredients of interest to the chemical andpharmaceutical industries. Pharmaceutical Substances is an invaluableresource for anybody involved in the design, discovery, development, andevaluation of drugs.

Pharmaceutical Substances was developed by Axel Kleemannand Jürgen Engel, as a solution to the problems they encountered whencreating their own bibliography for laboratory research. As a resultthese two great research chemists have brought together items ofinformation that, in their experience, are used day-in-day-out bypharmaceutical chemists. Together with their co-authors, BernhardKutscher and Dietmar Reichert they have created an indispensable toolfor researchers.

Pharmaceutical Substances is a first point of reference for any personwishing to screen references to drugs before turning to more detailedprimary literature, such as the original patent application or theoriginal research paper. Extensive indexing and cross linking ofreferences provides the reader with a fast and easy way to comparepharmaceutical ingredients with similar characteristics.

All compounds are organized alphabetically according totheir International Nonproprietary Name (INN). For added ease of use thebook features 4 additional indexes:

  • Intermediates
  • Trade Names
  • Enzymes, Microorganisms, Plants and Animal Tissues
  • Substance Classes

The description of each compound includes:

  • Chemical structure
  • Graphical representation of synthetic route includingintermediates
  • Nomenclature: INN standard, trivial names, synonyms,CAS number
  • ATC codes
  • Medical applications/Therapeutic category
  • Toxicological data
  • Patent number, origin, holder and date of application
  • Commercial information
  • Bibliographic information including CASSI codes

Editorial Review

Soon available.

The Organic Chemistry of Drug Design and Drug Action

Richard Silverman

Hardcover, 617 Pages
2nd Edition, 2004
ISBN: 0-12-643732-7
Academic Press


Standard medicinal chemistry courses and texts are organized by classes ofdrugs with an emphasis on descriptions of their biological and pharmacologicaleffects. This book represents a new approach based on physical organic chemicalprinciples and reaction mechanisms that rationalize drug action and allow thereader to extrapolate to many related classes of drug molecules. The SecondEdition reflects the significant changes in the drug industry over the pastdecade, and now includes color illustrations, chapter problems, and otherelements that make concepts easier to understand.

Editorial Review

"The Organic Chemistry of Drug Design andDrug Action" is a comprehensive monograph that is suitable for bothadvanced students and PhDs alike who have not yet become acquainted withthe area, but who wish to prepare themselves for a career in drugresearch.

What stands out in comparison with otherbooks discussed here is that the subjects are generally addressed indetail, and each theoretical point is illustrated with examples ofspecific drugs. A great deal of knowledge is reflected in the structurespresented. Key learnings as to which drug properties are obtainedthrough specific, individual modifications are presented, based uponexamples with detailed rationale. Collectively, these represent animmense body of knowledge that is built up from empirical data. Theauthor provides an extensive discussion of drug candidate optimizationwithout the aid of molecular modeling, wherein the approaches presentedare logically based and thus quite accessible to the reader. "TheOrganic Chemistry of Drug Design and Drug Action" offers valuable andin-depth suggestions concerning many facets of drug discovery.

Moreover, this volume is worthwhile readingfor the several detailed chapters of historical interest that itcontains, although this material is still placed in context with thebiochemical principles underlying the structures presented. Even thechapter on "DNA-Interactive Agents" is remarkably useful, although thereader may be excused for not committing all of the examples to memory.

The recommendation for those with aninterest in medicinal chemistry is to obtain an introductory textbook,and by all means to acquire "The Organic Chemistry of Drug Design andDrug Action" as the advanced text. Even if Silverman’s book foregoes anyvivid treatment of molecular modeling or the involvement of manybiochemical principles, readers will gain a deeper understanding fromthe concrete examples and excellent commentaries provided.


Drug Discovery, Design, and Development
Enzymes (Catalytic Receptors)
Enzyme Inhibition and Inactivation
DNA-Interactive Agents
Drug Metabolism
Prodrugs and Drug Delivery Systems

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