Progress in Drug Research, C.G. Halford; J.E. Blundell; S. Ren; E.J. Lien; B.

Автор: Golan, David E.
Название: Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy
ISBN: 1496320573 ISBN-13(EAN): 9781496320575
Издательство: Lippincott Williams & Wilkins
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Цена: 59670.00 T
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Описание: Highly regarded by both students and instructors, Principles of Pharmacology: The Pathophysiologic Basis of Drug Therapy, 4th Edition, offers an integrated mechanism-based and systems-based approach to contemporary pharmacology and drug development.

Автор: Bernard Testa
Название: Hydrolysis in Drug and Prodrug Metabolism: Chemistry, Biochemistry, and Enzymology
ISBN: 390639025X ISBN-13(EAN): 9783906390253
Издательство: Wiley
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Цена: 158400.00 T
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Описание: In this volume, Professor Bernard Testa and Dr Joachim Mayer discuss the molecular and biochemical aspects of metabolic reactions of hydrolysis and hydration. While an encyclopaedic treatment is avoided, the covered topics include biochemicproperties of the enzymes/isozymes, drug-enzyme interactions, the various chemical reactions catalyzed by the enzyme(s), reaction mechanisms and catalytic cycles, regio- and stereoselectivities, structure-metabolism relationships, molecular aspects of toxication and detoxication, as well as enzyme inhibition. The classification of matters is based mainly on the types of target groups and compounds being transformed, with carefully selected examples illustrating the reactions under discussion. Such a treatment has heuristic value since it renders the reader capable of educated guesses on the metabolism of other or novel drugs.

Автор: Lars Bohlin; Jan G. Bruhn
Название: Bioassay Methods in Natural Product Research and Drug Development
ISBN: 9401060193 ISBN-13(EAN): 9789401060196
Издательство: Springer
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Цена: 174150.00 T
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Описание: Bioassay Methods in Natural Product Research and Drug Development contains the proceedings from the Phytochemical Society of Europe`s very successful symposium on this topic, held August 24-27, 1997 in Uppsala, Sweden.

Автор: Bernard Testa
Название: Pharmacokinetic Optimization in Drug Research: Biological, Physicochemical, and Computational Strategies
ISBN: 3906390225 ISBN-13(EAN): 9783906390222
Издательство: Wiley
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Цена: 153120.00 T
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Описание: In this age of combinatorial chemistry and high-throughput technologies, bioactive compounds called hits are discovered by the thousands. However, the road that leads from hits to lead compounds and then to pharmacokinetically optimized clinical and drug candidates is very long indeed. 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 develop-ment and high rate of attrition of active compounds ultimately doomed by hidden pharmacokinetic defects, drug researchers are coming to incorporate structure-permeation, structure-distribution, structure-metabolism, and structure-toxicity relations into drug-design strategies. To this end, 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. Toxicological issues are also of utmost importance in this paradigm. There was, hence, an urgent need for a book covering this field in an authoritative, didactic, comprehensive, factual, and conceptual manner. In this work of unique breadth and depth, international authorities and practicing experts from academia and industry present the most modern biological, physicochemical, and computational strategies to optimize gastrointestinal absorption, protein binding and distribution, brain permeation, and metabolic profile. The biological strategies emphasized in the book include cell cultures and high-throughput screens. The physicochemical strategies focus on the determination and interpretation of solubility, lipophilicity, and related molecular properties as factors and predictors of pharmacokinetic bahavior. Particular attention is paid to the lipophilicity profiles of ionized compounds, to lipophicity measurements in anisotropic media (liposomes/water, IAM columns), and to permeability across artificial membranes. Computational strategies comprise virtual screening, molecular modelling, lipophilicity, and H-bonding fields and their importance for structure-disposition relations. This book is both about theoretical and technological breakthroughs. Thus, molecular properties are contemplated from a dual perspective, namely a) their interpretation in biological and/or physicochemical terms, and b) their value in screening, lead optimization, and drug-candidate selection. In addition to its 33 chapters, the book includes a CD-ROM containing the invited lectures, oral communications and posters (in full version) presented at the Second LogP Symposium, 'Lipophilicity in Drug Disposition -- Practical and Computational Approaches to Molecular Properties Related to Drug Permeation, Disposition and Metabolism', held at the University of Lausanne in March 2000.

Автор: Bernard Testa
Название: Pharmacokinetic Profiling in Drug Research: Biological, Physicochemical, and Computational Strategies
ISBN: 3906390357 ISBN-13(EAN): 9783906390352
Издательство: Wiley
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Цена: 239660.00 T
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Описание: 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.

Автор: G.A. Jeffrey; J.F. Piniella
Название: The Application of Charge Density Research to Chemistry and Drug Design
ISBN: 1461366453 ISBN-13(EAN): 9781461366454
Издательство: Springer
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Цена: 81050.00 T
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Описание: Proceedings of a NATO ASI, held in Sant Feluide Guixols, Costa Brava, Spain, April 17--27, 1990