Privileged Structures In Drug Discovery
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Author | : Larry Yet |
Publisher | : John Wiley & Sons |
Total Pages | : 562 |
Release | : 2018-03-07 |
Genre | : Medical |
ISBN | : 1118686357 |
A comprehensive guide to privileged structures and their application in the discovery of new drugs The use of privileged structures is a viable strategy in the discovery of new medicines at the lead optimization stages of the drug discovery process. Privileged Structures in Drug Discovery offers a comprehensive text that reviews privileged structures from the point of view of medicinal chemistry and contains the synthetic routes to these structures. In this text, the author—a noted expert in the field—includes an historical perspective on the topic, presents a practical compendium to privileged structures, and offers an informed perspective on the future direction for the field. The book describes the up-to-date and state-of-the-art methods of organic synthesis that describe the use of privileged structures that are of most interest. Chapters included information on benzodiazepines, 1,4-dihydropyridines, biaryls, 4-(hetero)arylpiperidines, spiropiperidines, 2-aminopyrimidines, 2-aminothiazoles, 2-(hetero)arylindoles, tetrahydroisoquinolines, 2,2-dimethylbenzopyrans, hydroxamates, and bicyclic pyridines containing ring-junction nitrogen as privileged scaffolds in medicinal chemistry. Numerous, illustrative case studies document the current use of the privileged structures in the discovery of drugs. This important volume: Describes the drug compounds that have successfully made it to the marketplace and the chemistry associated with them Offers the experience from an author who has worked in many therapeutic areas of medicinal chemistry Details many of the recent developments in organic chemistry that prepare target molecules Includes a wealth of medicinal chemistry case studies that clearly illustrate the use of privileged structures Designed for use by industrial medicinal chemists and process chemists, academic organic and medicinal chemists, as well as chemistry students and faculty, Privileged Structures in Drug Discovery offers a current guide to organic synthesis methods to access the privileged structures of interest, and contains medicinal chemistry case studies that document their application.
Author | : Stefan Bräse |
Publisher | : Royal Society of Chemistry |
Total Pages | : 486 |
Release | : 2015-11-20 |
Genre | : Medical |
ISBN | : 1782620303 |
This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.
Author | : Andrea Basso |
Publisher | : Frontiers Media SA |
Total Pages | : 150 |
Release | : 2019-03-22 |
Genre | : |
ISBN | : 2889457885 |
Has the concept of Diversity Oriented Synthesis remained unchanged over these two decades, or do we observe improvements or deviations from the original guidelines drawn by the pioneers? The aim of this Research Topic is to collect contributions on the state-of-the-art and progress of Diversity Oriented Synthesis, and to foresee its shape in the next decade.
Author | : Jean-Paul Renaud |
Publisher | : John Wiley & Sons |
Total Pages | : 1437 |
Release | : 2020-01-09 |
Genre | : Medical |
ISBN | : 1118900502 |
With the most comprehensive and up-to-date overview of structure-based drug discovery covering both experimental and computational approaches, Structural Biology in Drug Discovery: Methods, Techniques, and Practices describes principles, methods, applications, and emerging paradigms of structural biology as a tool for more efficient drug development. Coverage includes successful examples, academic and industry insights, novel concepts, and advances in a rapidly evolving field. The combined chapters, by authors writing from the frontlines of structural biology and drug discovery, give readers a valuable reference and resource that: Presents the benefits, limitations, and potentiality of major techniques in the field such as X-ray crystallography, NMR, neutron crystallography, cryo-EM, mass spectrometry and other biophysical techniques, and computational structural biology Includes detailed chapters on druggability, allostery, complementary use of thermodynamic and kinetic information, and powerful approaches such as structural chemogenomics and fragment-based drug design Emphasizes the need for the in-depth biophysical characterization of protein targets as well as of therapeutic proteins, and for a thorough quality assessment of experimental structures Illustrates advances in the field of established therapeutic targets like kinases, serine proteinases, GPCRs, and epigenetic proteins, and of more challenging ones like protein-protein interactions and intrinsically disordered proteins
Author | : Li Di |
Publisher | : Elsevier |
Total Pages | : 549 |
Release | : 2010-07-26 |
Genre | : Science |
ISBN | : 0080557619 |
Of the thousands of novel compounds that a drug discovery project team invents and that bind to the therapeutic target, typically only a fraction of these have sufficient ADME/Tox properties to become a drug product. Understanding ADME/Tox is critical for all drug researchers, owing to its increasing importance in advancing high quality candidates to clinical studies and the processes of drug discovery. If the properties are weak, the candidate will have a high risk of failure or be less desirable as a drug product. This book is a tool and resource for scientists engaged in, or preparing for, the selection and optimization process. The authors describe how properties affect in vivo pharmacological activity and impact in vitro assays. Individual drug-like properties are discussed from a practical point of view, such as solubility, permeability and metabolic stability, with regard to fundamental understanding, applications of property data in drug discovery and examples of structural modifications that have achieved improved property performance. The authors also review various methods for the screening (high throughput), diagnosis (medium throughput) and in-depth (low throughput) analysis of drug properties. - Serves as an essential working handbook aimed at scientists and students in medicinal chemistry - Provides practical, step-by-step guidance on property fundamentals, effects, structure-property relationships, and structure modification strategies - Discusses improvements in pharmacokinetics from a practical chemist's standpoint
Author | : Steven Howard |
Publisher | : Royal Society of Chemistry |
Total Pages | : 314 |
Release | : 2015-06-17 |
Genre | : Medical |
ISBN | : 1782625658 |
Fragment-based drug discovery is a rapidly evolving area of research, which has recently seen new applications in areas such as epigenetics, GPCRs and the identification of novel allosteric binding pockets. The first fragment-derived drug was recently approved for the treatment of melanoma. It is hoped that this approval is just the beginning of the many drugs yet to be discovered using this fascinating technique. This book is written from a Chemist's perspective and comprehensively assesses the impact of fragment-based drug discovery on a wide variety of areas of medicinal chemistry. It will prove to be an invaluable resource for medicinal chemists working in academia and industry, as well as anyone interested in novel drug discovery techniques.
Author | : Lisa B. English |
Publisher | : Springer Science & Business Media |
Total Pages | : 380 |
Release | : 2008-02-04 |
Genre | : Science |
ISBN | : 1592592856 |
The continued successes of large- and small-scale genome sequencing projects are increasing the number of genomic targets available for drug d- covery at an exponential rate. In addition, a better understanding of molecular mechanisms—such as apoptosis, signal transduction, telomere control of ch- mosomes, cytoskeletal development, modulation of stress-related proteins, and cell surface display of antigens by the major histocompatibility complex m- ecules—has improved the probability of identifying the most promising genomic targets to counteract disease. As a result, developing and optimizing lead candidates for these targets and rapidly moving them into clinical trials is now a critical juncture in pharmaceutical research. Recent advances in com- natorial library synthesis, purification, and analysis techniques are not only increasing the numbers of compounds that can be tested against each specific genomic target, but are also speeding and improving the overall processes of lead discovery and optimization. There are two main approaches to combinatorial library production: p- allel chemical synthesis and split-and-mix chemical synthesis. These approaches can utilize solid- or solution-based synthetic methods, alone or in combination, although the majority of combinatorial library synthesis is still done on solid support. In a parallel synthesis, all the products are assembled separately in their own reaction vessels or microtiter plates. The array of rows and columns enables researchers to organize the building blocks to be c- bined, and provides an easy way to identify compounds in a particular well.
Author | : Gisbert Schneider |
Publisher | : John Wiley & Sons |
Total Pages | : 540 |
Release | : 2013-10-10 |
Genre | : Medical |
ISBN | : 3527677038 |
Systematically examining current methods and strategies, this ready reference covers a wide range of molecular structures, from organic-chemical drugs to peptides, Proteins and nucleic acids, in line with emerging new drug classes derived from biomacromolecules. A leader in the field and one of the pioneers of this young discipline has assembled here the most prominent experts from across the world to provide first-hand knowledge. While most of their methods and examples come from the area of pharmaceutical discovery and development, the approaches are equally applicable for chemical probes and diagnostics, pesticides, and any other molecule designed to interact with a biological system. Numerous images and screenshots illustrate the many examples and method descriptions. With its broad and balanced coverage, this will be the firststop resource not only for medicinal chemists, biochemists and biotechnologists, but equally for bioinformaticians and molecular designers for many years to come. From the content: * Reaction-driven de novo design * Adaptive methods in molecular design * Design of ligands against multitarget profiles * Free energy methods in ligand design * Fragment-based de novo design * Automated design of focused and target family-oriented compound libraries * Molecular de novo design by nature-inspired computing * 3D QSAR approaches to de novo drug design * Bioisosteres in de novo design * De novo design of peptides, proteins and nucleic acid structures, including RNA aptamers and many more.
Author | : János Fischer |
Publisher | : John Wiley & Sons |
Total Pages | : 258 |
Release | : 2015-05-04 |
Genre | : Medical |
ISBN | : 3527336850 |
The first volume of the book series "Successful Drug Discovery" is focusing on new drug discoveries during the last decade, from established drugs to recently introduced drugs of all kinds: small-molecule-, peptide-, and protein-based drugs. The role of serendipity is analyzed in some very successful drugs where the research targets of the lead molecule and the drug are different. Phenotypic and target-based drug discovery approaches are discussed from the viewpoint of pioneer drugs and analogues. This volume gives an excellent overview of insulin analogues including a discussion of the properties of rapid-acting and long-acting formulations of this important hormone. The major part of the book is devoted to case histories of new drug discoveries described by their key inventors. Eight case histories range across many therapeutic fields. The goal of this book series is to help the participants of the drug research community with a reference book series and to support teaching in medicinal chemistry with case histories and review articles of new drugs.
Author | : Om Silakari |
Publisher | : Elsevier |
Total Pages | : 438 |
Release | : 2018-06-11 |
Genre | : Science |
ISBN | : 0081021054 |
Key Heterocycle Cores for Designing Multitargeting Molecules provides a helpful overview of current developments in the field. Following a detailed introduction to the manipulation of heterocycle cores for the development of dual or multitargeting molecules, the book goes on to describe specific examples of such developments, focusing on compounds such as Benzimidazole, Acridine, Flavones, Thiazolidinedione and Oxazoline. Drawing on the latest developments in the field, this volume provides a valuable guide to current approaches in the design and development of molecules capable of acting on multiple targets. Adapting the heterocyclic core of a single-target molecule can facilitate its development into an agent capable of acting on multiple targets. Such multi-targeting drugs have the potential to become essential components in the design of novel, holistic treatment plans for complex diseases, making the design of such active agents an increasingly important area of research. - Emphasizes the chemical development of heterocyclic nuclei, from single to multitargeting molecules - Provides chapter-by-chapter coverage of the key heterocyclic compounds used in synthesizing multitargeting agents - Outlines current trends and future developments in multitarget molecule design for the treatment of various diseases