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Organic Stereochemistry - Guiding Principles and Biomedicinal Relevance (Paperback): Bernard Testa, John Caldwell, M.Volkan... Organic Stereochemistry - Guiding Principles and Biomedicinal Relevance (Paperback)
Bernard Testa, John Caldwell, M.Volkan Kisakurek
R1,859 R1,533 Discovery Miles 15 330 Save R326 (18%) Shipped within 7 - 12 working days

""This book should become an indispensable asset on the bookshelves of pharmaceutical laboratories in academia and in industry, as well as of laboratories devoted to plant protection. I am convinced that studying this book will be an eye-opener for many scientists in the field of life sciences. Furthermore, for teachers in this area it will not only be a useful compilation of the various languages and definitions of organic stereochemistry, but also a welcome source of examples for demonstrating to their students the intricate and intriguing role stereochemistry plays in the chemistry of life."" -Prof. Dr. Dieter Seebach, Laboratory of Organic Chemistry, ETH Zurich, Switzerland

This textbook presents the molecular scale of matter in the broad diversity and richness of its three dimensions, giving due attention when relevant to the temporal dimension in which molecules exist, act, and react.

The focus is on two significant fields of three-dimensional chemistry: a presentation of the guiding principles in organic stereochemistry, followed by a focus on the biochemical and medicinal relevance of this discipline.

The treatment of "Guiding Principles "gives priority to didactic clarity and nomenclature issues, as detailed and illustrated in Parts 1 to 4: '"Symmetry Elements and Operations, Classification of Stereoisomers"''"Stereoisomerism Resulting from One or Several Stereogenic Centers"''"Other Stereogenic Elements: Axes of Chirality, Planes of Chirality, Helicity, and ("E," "Z")-Diastereoisomerism"''"Isomerisms about Single Bonds and in Cyclic Systems"'

This is followed by Parts 5 to 8 which focus on the biomedicinal relevance of stereochemistry, with special reference to the biochemistry and pharmacology of medicinal compounds.

Here, examples and applications are discussed and illustrated based on their relevance to a given specific stereochemical aspect: '"Chirality in Molecular and Clinical Pharmacology"''"The Conformational Factor in Molecular Pharmacology"''"The Concept of Substrate Stereoselectivity in Biochemistry and Xenobiotic Metabolism"''"Prostereoisomerism and the Concept of Product Stereoselectivity in Xenobiotic Metabolism"'

Finally, the book contains a gift for broad-minded readers with an interest in the historical roots of stereochemistry: Part 9: '"Molecular Chirality in Chemistry and Biology: Historical Milestones"'

Key features: Consists entirely of beautifully produced colored figuresIncludes marginal notes, giving clear-cut short definitions of terms used in the corresponding captionProvides an alphabetic glossary of termsOffers an extensive index

The The Biochemistry of Drug Metabolism, v. 1 - The Biochemistry of Drug Metabolism Principles, Redox Reactions, Hydrolyses... The The Biochemistry of Drug Metabolism, v. 1 - The Biochemistry of Drug Metabolism Principles, Redox Reactions, Hydrolyses (Paperback)
Bernard Testa, Stefanie D. Kramer
R1,825 R1,519 Discovery Miles 15 190 Save R306 (17%) Shipped within 7 - 12 working days

The first of the two volumes is divided into three parts. Part One begins by introducing xenobiotics in the broad context of physiological metabolism, and continues with an overview of the processes of drug disposition and metabolism. It then goes on to summarize the macroscopic and microscopic locations of drug metabolism in animals and humans. This is followed by an introduction to the all-important issue of the consequences of drug and xenobiotic metabolism, providing an initial overview of pharmacokinetic, pharmacological and toxicological consequences. The last chapter examines drug metabolism in the context of drug research, with a focus on medicinal chemistry.
The second part is a major component of the book, corresponding to the role of oxidoreductases as major agents of metabolism. Cytochromes P450 receive particular attention, namely their multiplicity, structure, catalytic mechanisms, and the various reactions they catalyze, while other oxidoreductases are also presented, such as flavin monooxygenases, monoamine oxidases and other amine oxidases, aldehyde oxidase and xanthine dehydrogenase, peroxidases, and dehydrogenases-reductases. Each drug-metabolizing enzyme or enzyme family begins with an Enzyme Identity Card summarizing its nomenclature and biochemical essentials.
Part Three begins with a survey of the classification, properties and catalytic mechanism of the innumerable hydrolases known or suspected to play a role in xenobiotic metabolism. The focus then shifts to a systematic presentation of the various substrate classes, namely carboxylic esters, amides and peptides, lactams and lactones, esters of inorganic acids, alkene and arene epoxides, and some miscellaneous hydrolyzable moieties.
With a foreword by Prof Leslie Z. Benet, the world's best and best-known biopharmaceutical scientist

The The Biochemistry of Drug Metabolism, v. 2 - The Biochemistry of Drug Metabolism Conjugations, Consequences of Metabolism,... The The Biochemistry of Drug Metabolism, v. 2 - The Biochemistry of Drug Metabolism Conjugations, Consequences of Metabolism, Influencing Factors (Paperback)
Bernard Testa, Stefanie D. Kramer
R1,290 R1,172 Discovery Miles 11 720 Save R118 (9%) Shipped within 7 - 12 working days

Volume Two contains the last four parts of this work. Part 4 is devoted to the huge field of conjugation reactions, with much information being given on transferases. As in the two preceding parts, each drug-metabolizing enzyme or enzyme family begins with an Enzyme Identity Card summarizing its nomenclature and biochemical essentials. The reactions examined here include methylation, sulfation, glucuronidation, acetylation, conjugation with glutathione, while there is also a rigorous presentation of the pivotal role of xenobiotic-coenzyme A conjugates as a crossroads to various metabolic reactions.
The next part examines the consequences of drug and xenobiotic metabolism in a pharmacological and toxicological perspective, with due attention paid to full activation, as is found with prodrugs, and to the worrying case of xenobiotic toxification.
Parts 6 and 7 cover the inter-individual and intra-individual factors that influence drug metabolism, starting with an introduction to evolutionary events leading to species differences in the metabolism of xenobiotics and to polymorphisms within a particular species. Focusing on humans, the most relevant polymorphic drug-metabolizing enzymes are discussed, concentrating on ethnic differences and on the consequences for the pharmacokinetic behavior of affected drugs, while also introducing sex-dependent metabolic reactions.
The final part introduces the mechanisms leading to increases or decreases in enzyme activities as the concept of enzyme induction via nuclear receptors and the different mechanisms of enzyme inhibition are explained. With these basics in mind, various influencing factors are discussed, including physiological and pathological conditions, as well as drugs, nutrients and environmental agents with a special focus on drug-drug interactions.
With a foreword by Prof Leslie Z. Benet -- the best and best-known biopharmaceutical scientist worldwide.

Drug Bioavailability - Estimation of Solubility, Permeability, Absorption and Bioavailability (Hardcover, 2nd Edition): Han Van... Drug Bioavailability - Estimation of Solubility, Permeability, Absorption and Bioavailability (Hardcover, 2nd Edition)
Han Van De Waterbeemd, Bernard Testa; Series edited by Raimund Mannhold, Hugo Kubinyi, Gerd Folkers
R4,451 R3,956 Discovery Miles 39 560 Save R495 (11%) Shipped within 7 - 12 working days

The gold standard for industrial research now completely revised in line with current trends in the field, with all contributions extensively updated or rewritten.
In 21 chapters readers can benefit from the key working knowledge of today's leading pharmaceutical companies, including Pfizer, AstraZeneca, and Roche. Drug developers from industry and academia present all the factors governing drug bioavailability, complete with practical examples and real-life data.
Part I focuses on in vitro and in vivo measurements of physicochemical properties, such as membrane permeability and ionization. Part II discusses solubility and gastrointestinal absorption, while the third part is devoted to metabolism and excretory mechanisms. The much revised and expanded part IV surveys current in silico approaches to predict drug properties needed to estimate the bioavailability of any new drug candidate. The final part shows how poor bioavailability may be improved by various approaches during the development process.
No other publication offers the same level of treatment on this crucial topic in modern drug development.

Pharmacokinetic Profiling in Drug Research - Biological, Physicochemical, and Computational Strategies (Hardcover): Bernard... Pharmacokinetic Profiling in Drug Research - Biological, Physicochemical, and Computational Strategies (Hardcover)
Bernard Testa, Stefanie D. Kramer, Heidi Wunderli-Allenspach, Gerd Folkers
R4,451 R3,956 Discovery Miles 39 560 Save R495 (11%) Shipped within 7 - 12 working days

Informatics and robotics are the workhorses of a technological revolution in drug research. On them are based combinatorial chemistry, which yields compounds by the many thousands, and high-throughput bioassays, which screen them for activity. The results are avalanches of 'hits', which invade the databases like swarms of locusts. But far from being a plague, these innumerable compounds become a blessing if properly screened for 'drugability', i.e., for 'drug-like' properties such as good pharmacokinetic (PK) behavior. Pharmacokinetic profiling of bioactive compounds has, thus, become a sine qua non condition for cherry-picking the most promising hits. Just as important, but less visible, are the structure-property and structure-ADME relations, which emerge from PK profiling and provide useful feedback when designing new synthetic series. As a result, the screening, design, and optimization of pharmacokinetic properties has become the bottleneck and a major challenge in drug research. To shorten the time-consuming development and high rate of attrition of active compounds ultimately doomed by hidden pharmacokinetic defects, powerful biological, physicochemical, and computational approaches are being developed, whose objectives are to increase the clinical relevance of drug design and to eliminate as soon as possible compounds with unfavorable physicochemical properties and pharmacokinetic profiles.
The profiling of ADME properties (absorption, distribution, metabolism, and excretion) is the topic of this book. Following the extraordinary success of the previous work ('Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical, and Computational Strategies', Eds. B. Testa, H. van de Waterbeemd, G. Volkers, R. Guy, Verlag Helvetica Chimica Acta, Zurich, 2001, 655 pages), there was a need for an essentially new edition focusing on the latest theoretical and technological breakthroughs. In this unique work, international authorities and practicing experts from academia and industry offer state-of-the-art presentations of concepts, methods and technologies now in use or development in drug research. The biological strategies emphasized in the book include cell cultures, drug-metabolizing enzymes, transporters and plasma protein binding. The physicochemical strategies focus on artificial membrane-permeability assays, on solubility and lipophilicity and related molecular properties as factors and predictors of pharmacokinetic behavior, and on stability and solid-state properties. Computational strategies comprize the exploration of property spaces, pharmacophore searching to predict biotransformation and enzyme inhibition, and expert systems to process biopharmaceutical profiling data.
In addition to its 28 chapters, the book includes a CD-ROM containing the invited lectures, oral communications, and posters (in full version) presented at the Third LogP Symposium, 'Physicochemical and Biological Profiling in Drug Research', held at the Federal Institute of Technology (ETH) of Zurich in March 2004.

The Biochemistry of Drug Metabolism - Principles, Redox Reactions, Hydrolyses, Two Volume Set (Paperback): Bernard Testa,... The Biochemistry of Drug Metabolism - Principles, Redox Reactions, Hydrolyses, Two Volume Set (Paperback)
Bernard Testa, Stefanie D. Kramer
R2,707 R1,928 Discovery Miles 19 280 Save R779 (29%) Shipped within 7 - 13 working days

Offering a conceptual and factual presentation of the metabolism of drugs and other xenobiotics, these two volumes distinctly focus on the biochemistry, with an emphasis on xenobiotic-metabolizing enzymes, their reactions and regulations.
The first volume is divided into three parts. Part One begins by introducing xenobiotics in the broad context of physiological metabolism, and continues with an overview of the processes of drug disposition and metabolism. It then goes on to summarize the macroscopic and microscopic locations of drug metabolism in animals and humans. This is followed by an introduction to the all-important issue of the consequences of drug and xenobiotic metabolism, providing an initial overview of pharmacokinetic, pharmacological and toxicological consequences. The last chapter examines drug metabolism in the context of drug research, with a focus on medicinal chemistry.
The second part is a major component of the book, corresponding to the role of oxidoreductases as major agents of metabolism. Cytochromes P450 receive particular attention, namely their multiplicity, structure, catalytic mechanisms, and the various reactions they catalyze, while other oxidoreductases are also presented, such as flavin monooxygenases, monoamine oxidases and other amine oxidases, aldehyde oxidase and xanthine dehydrogenase, peroxidases, and dehydrogenases-reductases. Each drug-metabolizing enzyme or enzyme family begins with an Enzyme Identity Card summarizing its nomenclature and biochemical essentials.
Part Three begins with a survey of the classification, properties and catalytic mechanism of the innumerable hydrolases known or suspected to play a role in xenobiotic metabolism. The focus then shifts to a systematic presentation of the various substrates classes, namely carboxylic esters, amides and peptides, lactams and lactones, esters of inorganic acids, alkene and arene epoxides, and some miscellaneous hydrolyzable moieties.
Volume Two contains the last four parts of this work. Part 4 is devoted to the huge field of conjugation reactions, with much information being given on transferases. As in the two preceding parts, each drug-metabolizing enzyme or enzyme family begins with an Enzyme Identity Card summarizing its nomenclature and biochemical essentials. The reactions examined here include methylation, sulfation, glucuronidation, acetylation, conjugation with glutathione, while there is also a rigorous presentation of the pivotal role of xenobiotic-coenzyme A conjugates as a crossroads to various metabolic reactions.
The next part examines the consequences of drug and xenobiotic metabolism in a pharmacological and toxicological perspective, with due attention paid to full activation, as is found with prodrugs, and to the worrying case of xenobiotic toxification.
Parts 6 and 7 cover the inter-individual and intra-individual factors that influence drug metabolism, starting with an introduction to evolutionary events leading to species differences in the metabolism of xenobiotics and to polymorphisms within a particular species. Focusing on humans, the most relevant polymorphic drug-metabolizing enzymes are discussed, concentrating on ethnic differences and on the consequences for the pharmacokinetic behavior of affected drugs, while also introducing sex-dependent metabolic reactions.
The final part introduces the mechanisms leading to increases or decreases in enzyme activities as the concept of enzyme induction via nuclear receptors and the different mechanisms of enzyme inhibition are explained. With these basics in mind, various influencing factors are discussed, including physiological and pathological conditions, as well as drugs, nutrients and environmental agents with a special focus on drug-drug interactions.
With a foreword by Prof Leslie Z. Benet, the renowned biopharmaceutical scientist.

Advances in Drug Research, Volume 28 (Hardcover): Bernard Testa, Urs A. Meyer Advances in Drug Research, Volume 28 (Hardcover)
Bernard Testa, Urs A. Meyer
R2,425 Discovery Miles 24 250 Special order

This volume continues the trend for Advances in Drug Research of shorter, but more frequent volumes. In line with the tradition of the series, chapters on general themes are interspersed with chapters on specific drug classes and targets.

Biochemistry of Redox Reactions (Hardcover): Bernard Testa, John Caldwell Biochemistry of Redox Reactions (Hardcover)
Bernard Testa, John Caldwell
R4,489 Discovery Miles 44 890 Special order

Surpassing the 1976 book by Testa and Jenner, Drug Metabolism: Chemical and Biochemical Aspects (Dekker), this informative, up-to-date text includes the following features, unavailable elsewhere: First in a set of books to provide a comprehensive coverage of drug metabolism; Opening chapter provides a general introduction to the complete set of books; Other chapters cover reaction mechanisms, catalytic cycles, regio- and stereoselectivities, types of substrates, reactivity of intermediates, and drug-enzyme interactions; Extensive detailed diagrams of reaction pathways and chemical structures
* First in a set of books providing a comprehensive coverage of drug metabolism
* Opening chapter provides a general introduction to the complete set of books
* Other chapters cover reaction mechanisms, catalytic cycles, regio and stereoselectivities, types of substrates, reactivity of intermediates and drug-enzyme interactions
* Extensive detailed diagrams of reaction pathways and chemical structures

Advances in Drug Research, Volume 26 (Hardcover): Bernard Testa, Urs A. Meyer Advances in Drug Research, Volume 26 (Hardcover)
Bernard Testa, Urs A. Meyer
R1,198 Discovery Miles 11 980 Special order

Volume 26 continues the trend of shorter, more frequent volumes. With Volume 25, the series gained a new co-editor, Urs Meyer. While retaining the commitment to publish chapters on therapeutic or chemical classes and on general topics or concepts, the series' coverage has expanded to include methodological chapters, and new areas of recognized or potential significance to drug research, especially in molecular pharmacology.

Advances in Drug Research, Volume 29 (Hardcover): Bernard Testa, Urs A. Meyer Advances in Drug Research, Volume 29 (Hardcover)
Bernard Testa, Urs A. Meyer
R2,659 Discovery Miles 26 590 Special order

This volume continues the trend for Advances in Drug Research of shorter, but more frequent volumes. In line with the tradition of the series, chapters on general themes are interspersed with chapters on specific drug classes and targets.

Virtual ADMET Assessment in Target Selection and Maturation (Paperback, Illustrated Ed): Bernard Testa, L. Turski Virtual ADMET Assessment in Target Selection and Maturation (Paperback, Illustrated Ed)
Bernard Testa, L. Turski
R2,271 Discovery Miles 22 710 Special order

Today, biologists and medicinal chemists realize that there is a strong relationship between pharmacodynamic (what the drug does to the organism) and pharmacokinetic (what the organism does to the drug) effects. A significant contributing factor to the evolution in drug discovery was the methodological and technological revolution with the advent of combinatorial chemistry, high-throughput screening and profiling, and in silico prediction of target-based activity and ADMET (absorption, distribution, metabolism, excretion and toxicity) properties. High-throughput screening and in silico methods have accelerated the process towards drugability of new chemical structures. Another component of the revolution in drug discovery is the replacement of the disease (indication)-based approach by a target-based approach. A better understanding of pathophysiology of diseases and the underlying biological processes of diseases combined with explosive development of genomics and proteomics have been instrumental in the birth of this new paradigm. This volume summarizes discussions of these three aspects of modern drug discovery, i.e. priority for targets, early ADMET assessment, and in silico screening. We trust that readers from academia as well as from industry will benefit from these studies.

Antidiabetic Agents: Recent Advances in their Molecular and Clinical Pharmacology, Volume 27 (Hardcover): Bernard Testa, Urs A.... Antidiabetic Agents: Recent Advances in their Molecular and Clinical Pharmacology, Volume 27 (Hardcover)
Bernard Testa, Urs A. Meyer
R2,415 Discovery Miles 24 150 Special order

Volume 27, the first thematic volume in the Series, provides an overview of present knowledge with regard to the pharmacological and clinical aspects of antidiabetic drugs. It aims to stimulate further consideration of possible concepts in the development of new antidiabetic drugs.

Stereochemical Aspects of Drug Action and Disposition (Hardcover): Michel Eichelbaum, Bernard Testa, Andrew Somogyi Stereochemical Aspects of Drug Action and Disposition (Hardcover)
Michel Eichelbaum, Bernard Testa, Andrew Somogyi
R1,992 Discovery Miles 19 920 Special order

This book aims to guide and inspire drug researchers as they enter the 21st century. Stereochemistry is an essential dimension in pharmacology and should be understood as such by all drug researchers whatever their background. When used as probes or medicines, stereoisomeric drugs offer invaluable insights or innovative therapeutic strategies. The book spans the subject from the molecular to the clinical. The first section on chemical aspects contains chapters on chemical synthesis, analysis, natural products, chiral stability (racemezation) and physical properties. The second section is on experimental pharmacology, with chapters on drug-receptor interactions, chiral recognition, ion channels, and molecular toxicology. The third section focuses on drug disposition, with chapters on absorption, distribution, protein binding, metabolism and elimination. The final section is dedicated to regulatory and clinical aspects.

Stereochemical Aspects of Drug Action and Disposition (Paperback, Softcover reprint of the original 1st ed. 2003): Michel... Stereochemical Aspects of Drug Action and Disposition (Paperback, Softcover reprint of the original 1st ed. 2003)
Michel Eichelbaum, Bernard Testa, Andrew Somogyi
R1,706 Discovery Miles 17 060 Special order

State-of-the-Art Chirality Stereochemistry in general and chirality in particular have long been recog- nized as major structural factors influencing pharmacological activity and pharmacokinetic behavior. For more than a century, relevant information in these fields has been accumulating at an accelerating pace, leading to rationalizations, concepts and theories of increasing breadth and depth. Frequently, fundamental advances in stereochemical aspects of molecular pharmacology, drug disposition and pharmacochemistry have been translated into corresponding progress in clinical pharmacology and pharmacotherapy. There have been exceptions, however, since some extrapolations from the biochemical and in vitro situations to the in vivo human situation have proven premature. This notion resulted in the now appeased, but far from closed, debate regarding racemic versus enantiopure drugs, which saw some pro- ponents state that "in many cases, only one isomer contributes to the thera- peutic action while the other, the 'isomeric ballast', only contributes to the side effects and toxicity" (ARIENS 1986,1989,1992). Other authors, in contrast, have cautioned against hasty generalizations and advocated a more pragmatic, case- by-case and evidence-based view (CALDWELL 1995; DE CAMP 1989; SZELENYI et al. 1998; TESTA 1991; TESTA and TRAGER 1990; TESTA et al. 1993).

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