Strategies for Organic Drug Synthesis and Design, Daniel Lednicer

Автор: Patrick H. Toy (Editor), Yulin Lam (Editor)
Название: Solid-Phase Organic Synthesis: Concepts, Strategies, and applications
ISBN: 0470599146 ISBN-13(EAN): 9780470599143
Издательство: Wiley
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Цена: 142510.00 T
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Описание: Presents both the fundamental concepts and the most recent applications in solid-phase organic synthesis With its emphasis on basic concepts, Solid-Phase Organic Synthesis guides readers through all the steps needed to design and perform successful solid-phase organic syntheses.

Автор: Tietze, Lutz F.
Название: Domino Reactions: Concepts for Efficient Organic Synthesis
ISBN: 3527334327 ISBN-13(EAN): 9783527334322
Издательство: Wiley
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Цена: 158350.00 T
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Описание: The follow-up to the successful "Domino Reaction in Organic Synthesis", this ready reference brings up to date on the original concept. The chapters have been arranged according to the name of well-known transformations of the first step and in combination with the formed products.

Автор: Patrick Graham
Название: Introduction to Drug Synthesis
ISBN: 0198708432 ISBN-13(EAN): 9780198708438
Издательство: Oxford Academ
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Описание: An Introduction to Drug Synthesis explores the central role played by organic synthesis in the process of drug design and development - from the generation of novel drug structures to the improved efficiency of large scale synthesis.

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.