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This unique reference set provides a broad-based, in-depth presentation on angiotensin II receptors, from the genes that encode them to the responses they mediate in humans. The books emphasize known and potential therapeutic applications of the antagonists of angiotensin II receptors and the angiotensin-converting enzyme inhibitors. The molecular biology of angiotensin II receptors is reviewed, as are the biochemical effects mediated by angiotensin II receptors. This is the first publication to analyze in detail the structure-activity relationships for both peptide and nonpeptide angiotensin II receptor agonists and antagonists. It also presents the pharmacological effects mediated by angiotensin II receptors both in the periphery and in the brain. ... Read more

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The long-awaited volume on synthetic chemistry in the series "Methods and Principles in Medicinal Chemistry" is now available. In the pharmaceutical industry, computational methods play a major role in the discovery and development of new drugs. Yet, the SYNTHESIS of these compounds still remains the most crucial topic in drug design.

Written by an internationally renowned team of authors and editors from academia and industry, this volume describes all recent developments in organic synthetic methodology which are essential for pharmaceutical research. The most modern synthetic developments of pharmacologically interesting compounds (carbohydrates and nucleotides) as well as important synthetic methods such as combinatorial chemistry, solid-phase reactions, bioassisted organic synthesis and asymmetric synthesis are critically discussed.

Special emphasis is given to a hands-on practical approach which enables researchers to apply the featured methods immediately to their specific problems. Also, the detailed presentation of the topic and the selection of references will be of help to any researcher working in the laboratory.
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This is Volume 5: Chemotherapeutic Agents, of Burger's Medicinal Chemistry and Drug Discovery, 6th Edition. This new volume contains critical new chapters on Molecular Biology of Cancer, Synthetic Anti-angiogenic Agents and Selective Toxicities.

To purchase the entire 6 volume set, please refer to ISBN 0-471-37032-0. ... Read more

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'It is indeed the merit of Dr. Alan F. Casy to bring in these pages a clear and comprehensive view of medicinal stereochemistry, a discipline in which he has been active and successful for many years both as a teacher and a researcher. Written for graduate students and research workers in medicinal chemistry and pharmacology, this book will contribute significantly towards a better education of scientists by removing the fear of stereochemistry caused by ignorance, moderating the overconfidence of possible zealots, and outlining a broader context.'--from the foreword by Bernard Testa ... Read more

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The perceived lack of drug discovery productivity in recent times has led to much debate in the pharmaceutical/biotechnology industry as escalating R&D costs are not being matched by increased output. Few observers doubt that selecting the right targets, ie those which are critical to disease pathology and are 'druggable', is the best starting point for improved productivity.

The seven chapters of this volume describe recent progress towards drugs acting at a range of 'druggable' targets. One chapter addresses kinases, one covers an ion channel, two proteases are featured and three of the chapters cover G-protein coupled receptors, which has historically perhaps been the most fruitful area for medicinal chemists.

*Presents the latest research in the field of drug discovery
*Publishes on an annual basis to bring you the most innovative updates in medicinal chemistry
*Available as an online resource via ScienceDirect ... Read more

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This practice-oriented handbook surveys current knowledge on the prediction and prevention of adverse drug reactions related to off-target activity of small molecule drugs. It is unique in collating the current approaches into a single source, and includes several highly instructive case studies that may be used as guidelines on how to improve drug development projects.
With its large section on ADME-related effects, this is key knowledge for every drug developer. ... Read more

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Carbonic anhydrases (CAs) are zinc enzymes widespread throughout the plant and animal kingdom. Their inhibitors have been used in a number of therapeutic applications including glaucoma, epilepsy, gastric ulcers, neurological disorders and osteoporosis among others. They play a vital role in important physiological functions such as respiration, metabolism, and biosynthetic reactions such as gluconeogenesis and ureagenesis. Carbonic Anhydrase, Its Inhibitors and Activators provides a state-of-the-art overview of the developments in CA and CA inhibitor research and will be of great interest to medicinal chemists, pharmacologists and professionals involved in novel drug design. ... Read more

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Smith Kline Beecham Pharmaceuticals, Essex, UK. Provides authoritative accounts of recent advances in new drugs and in the application of new technologies. Discusses inhibitors in the influenza virus sialidase, small molecule fibrinogen antagonists as antithrombotic agents, and more. For researchers. Trim size: 8.5 x 6 inches. ... Read more

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Hardbound. In this volume, there are five reviews of topical subjects.The availability of drugs for the successful treatment of many diseases results in an increase in the number of people who live to their eighties and nineties at which time Alzheimer's disease is most prevalent.The steady progress which is being made in our understanding of this complex disease and in the development of drugs for its treatment are reviewed in Chapter 1. Chemotherapy of another disease which often resists treatment may have another weapon in its armoury if recent work on modifying a naturally occurring anticancer compound (camptothecin) succeeds in reducing its side-effects; recent efforts in this field (described in Chapter 2) may yield a drug of value in treating cancer of the colon and stomach.Transporting a drug molecule to a specific site of action continues to present a challenge.The use of phosphates and phosphonates to protect the drug from hydrolysis or o ... Read more

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This concise and fully up-to-date account of the effects of drugs on the nervous system begins with an introduction to the fundamental aspects of neuronal function and synaptic transmission. Subsequent chapters describe the pharmacology of the neuromuscular junction, the parasympathetic and sympathetic divisions of the autonomic nervous system, and the central nervous system. The text provides a full survey of the nature and localization of neurotransmitters and their pathways; the molecular biology and subtypes of receptors; and the effects, side effects, and clinical uses of drugs. Some familiarity with molecular structures is helpful in understanding the relationships between drug classes and their action, so this volume includes molecular structures of most of the compounds discussed, with an indication of their stereochemistry. Bridging the disciplines of pharmacology and neuroscience and bringing together some of the most exciting and challenging aspects of both subjects, Neuropharmacology is intended for advanced undergraduate and graduate students in the biological and medical sciences, as well as a handy reference for neuroscientists, neurologists, psychiatrists, and psychologists who use pharmacology in their everyday research and practice. ... Read more

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Vaso-occlusive disorders including unstable angina, myocardial infarction, transient ischemic attacks, stroke and peripheral artery disease remain the major sources of morbidity and mortality in western civilization. Platelet activation and resulting platelet aggregation play a major role in the pathogenesis of these thromboembolic diseases. Recognition of the contribution of platelets to the pathophysiology of cardiovascular disease has provided impetus for the continued search for new antiplatelet agents. Hence, over the past two decades many strategies have been evaluated in the search for efficacious mechanisms to reduce platelet function. The medical need for more efficacious antithrombotic drugs and the growing understanding of the role of platelets in vascular injury have catalyzed the extensive evaluation of novel approaches to control platelet function. Along these lines, the volume therefore provides an in-depth assessment of ongoing clinical trials, new and clinically established agents, and other developments in this rapidly developing field. ... Read more

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'It is indeed the merit of Dr. Alan F. Casy to bring in these pages a clear and comprehensive view of medicinal stereochemistry, a discipline in which he has been active and successful for many years both as a teacher and a researcher. Written for graduate students and research workers in medicinal chemistry and pharmacology, this book will contribute significantly towards a better education of scientists by removing the fear of stereochemistry caused by ignorance, moderating the overconfidence of possible zealots, and outlining a broader context.'--from the foreword by Bernard Testa ... Read more

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The spectacular advances of medicinal chemistry in the last few decades have been triggered by a greater understanding of cellular processes at the molecular level. The understanding of biochemical processes and diseases at molecular level has revolutionized the field. This volume summarizes recent developments in the area of biological inhibitors such as squalene epoxidase inhibitors, dual inhibitors of 5-lipoxygenase and cycloxgenase, inhibition of cholestrol biosynthesis, HIV proteinase inhibitors, nonpeptide antagonists at peptide receptors, and binding interaction of thyroid hormones. ... Read more

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This text/reference presents fundamental aspects of medicinal chemistry and contains comprehensive information on approximately 5,000 drugs currently in use, describing their therapeutic uses, their mechanisms of action, and their main side and harmful effects. Employs the latest World Health Organization (WHO) pharmacological classification and provides extensive information for drugs on WHO's latest list of basic or essential pharmaceuticals, including history: chemical, trade and generic names; chemical structure; obtention; physical and chemical properties; mechanisms of action; therapeutic uses; adverse reactions; biotransformation; chemical and pharmacological incompatibilities; bioavailability; dosage; storage; and assay. ... Read more

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Recent progress in high-throughput screening, combinatorial chemistry and molecular biology has radically changed the approach to drug discovery in the pharmaceutical industry. New challenges in synthesis result in new analytical methods. At present, typically 100,000 to one million molecules have to be tested within a short period and, therefore, highly effective screening methods are necessary for today's researchers - preparing and characterizing one compound after another belongs to the past. Intelligent, computer-based search agents are needed and "virtual screening" provides solutions to many problems. Such screening comprises innovative computational techniques designed to turn raw data into valuable chemical information and to assist in extracting the relevant molecular features.

This handbook is unique in bringing together the various efforts in the field of virtual screening to provide the necessary methodological framework for more effective research. Leading experts give a thorough introduction to the state of the art along with a critical assessment of both successful applications and drawbacks. The information collated here will be indispensable for experienced scientists, as well as novices, working in medicinal chemistry and related disciplines. ... Read more

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Monoclonal antibodies have had their impact on biomedical research for more than a decade. Besides their exuberant use as reagents, quite a number of diagnostic and therapeutic approaches have been followed, and an impressive number of technological improvements, e.g., humanization, recombinant miniantibodies, have been elaborated to strengthen the principle.With respect to clinical applications, the first generation of antibody "drugs" is yielding promising results while second and third generation antibody constructs are already underway. This book reviews the status of technological development and brings this into the perspective of clinical results. A rapidly growing amount of clinical data is collected in an expanding number of indications. Hence, the review of clinical study results has been grouped according to the fields of oncology and of chronic and acute inflammation. ... Read more