Author : Stefan Bräse
Publisher : Royal Society of Chemistry
Page : 486 pages
File Size : 12,69 MB
Release : 2015-11-20
Category : Medical
ISBN : 1782620303
This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.
Author : Larry Yet
Publisher : John Wiley & Sons
Page : 562 pages
File Size : 21,75 MB
Release : 2018-03-07
Category : 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 : Andrea Trabocchi
Publisher : Elsevier
Page : 358 pages
File Size : 13,97 MB
Release : 2019-11-23
Category : Science
ISBN : 0128183500
Small Molecule Drug Discovery: Methods, Molecules and Applications presents the methods used to identify bioactive small molecules, synthetic strategies and techniques to produce novel chemical entities and small molecule libraries, chemoinformatics to characterize and enumerate chemical libraries, and screening methods, including biophysical techniques, virtual screening and phenotypic screening. The second part of the book gives an overview of privileged cyclic small molecules and major classes of natural product-derived small molecules, including carbohydrate-derived compounds, peptides and peptidomimetics, and alkaloid-inspired compounds. The last section comprises an exciting collection of selected case studies on drug discovery enabled by small molecules in the fields of cancer research, CNS diseases and infectious diseases. The discovery of novel molecular entities capable of specific interactions represents a significant challenge in early drug discovery. Small molecules are low molecular weight organic compounds that include natural products and metabolites, as well as drugs and other xenobiotics. When the biological target is well defined and understood, the rational design of small molecule ligands is possible. Alternatively, small molecule libraries are being used for unbiased assays for complex diseases where a target is unknown or multiple factors contribute to a disease pathology. - Outlines modern concepts and synthetic strategies underlying the building of small molecules and their chemical libraries useful for drug discovery - Provides modern biophysical methods to screening small molecule libraries, including high-throughput screening, small molecule microarrays, phenotypic screening and chemical genetics - Presents the most advanced chemoinformatics tools to characterize the structural features of small molecule libraries in terms of chemical diversity and complexity, also including the application of virtual screening approaches - Gives an overview of structural features and classification of natural product-derived small molecules, including carbohydrate derivatives, peptides and peptidomimetics, and alkaloid-inspired small molecules
Author : Victor E. Marquez
Publisher : CRC Press
Page : 566 pages
File Size : 37,5 MB
Release : 2021-11-15
Category : Medical
ISBN : 1000462943
The Ups and Downs in Drug Design: Adventures in Medicinal Chemistry highlights the necessity for an integrative approach in medicinal chemistry and chemical biology. As medicinal chemistry is not a monolithic science, it is important to emphasize the other various disciplines that are required for successful drug design. This book presents the author’s own personal experience in this field and describes the "ups" and "downs" that come with drug discovery. It is an excellent companion text for graduate and postgraduate students who would like further insight into the parameters of drug design, including the challenges that come with the project. Key Features Illustrates "real-life" examples in medicinal chemistry Integrates the use of physical, chemical, and biological concepts that are important in drug design Highlights the "ups" and "downs" that come with drug discovery Aims to inspire students who may be struggling with the challenges and thought process in drug design Intends to be an excellent companion text for graduate and postgraduate students
Author : Nathan Brown
Publisher : John Wiley & Sons
Page : 440 pages
File Size : 29,86 MB
Release : 2013-11-06
Category : Medical
ISBN : 3527665161
This first systematic treatment of the concept and practice of scaffold hopping shows the tricks of the trade and provides invaluable guidance for the reader's own projects. The first section serves as an introduction to the topic by describing the concept of scaffolds, their discovery, diversity and representation, and their importance for finding new chemical entities. The following part describes the most common tools and methods for scaffold hopping, whether topological, shape-based or structure-based. Methods such as CATS, Feature Trees, Feature Point Pharmacophores (FEPOPS), and SkelGen are discussed among many others. The final part contains three fully documented real-world examples of successful drug development projects by scaffold hopping that illustrate the benefits of the approach for medicinal chemistry. While most of the case studies are taken from medicinal chemistry, chemical and structural biologists will also benefit greatly from the insights presented here.
Author : Bin Yu
Publisher : Elsevier
Page : 988 pages
File Size : 13,95 MB
Release : 2023-07-19
Category : Medical
ISBN : 044318612X
Privileged Scaffolds in Drug Discovery is the most complete and up-to-date work in the area. Covering a wide range of privileged structures, it is a perfect reference for scientists involved in targeted drug development. The editors recruited epserts from several prestigious Chinese institutions to cover the areas of antiviral drugs, chalcone, pyrimidine, (benz)imidazoles, natural product-derived privileged scaffolds, N-Sulfonyl carboxamides, kinase inhibitors, antitumor molecules, antineurodegenerative drugs, triazoles, oxazolidinone, indole and indoline scaffolds, tigliane diterpenoids, peptide and peptide-based drugs, quassinoids, and others including pseudonatural products, macrocycles, stable peptides and peptidomimetics. The book also explores scaffolds in drug molecules approved in recent years. Privileged Scaffolds in Drug Discovery is a complete reference for researchers in drug discovery and organic synthesis, in academic and corporate settings, who are investigating privileged structures upon which to base new drugs. Researchers in medicinal chemistry and chemical biology will also find the contents of this book valuable. - Provides wide coverage of privileged scaffolds in new drug discovery - Includes complex and diverse natural product scaffolds - Covers applications to peptides and peptide-based drugs
Author : Om Silakari
Publisher : Elsevier
Page : 438 pages
File Size : 49,56 MB
Release : 2018-06-11
Category : 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
Author : Andrea Basso
Publisher : Frontiers Media SA
Page : 150 pages
File Size : 11,70 MB
Release : 2019-03-22
Category :
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 : Brent R. Stockwell
Publisher : Columbia University Press
Page : 289 pages
File Size : 14,60 MB
Release : 2011-06-01
Category : Medical
ISBN : 0231525524
After more than fifty years of blockbuster drug development, skeptics are beginning to fear we are reaching the end of drug discovery to combat major diseases. In this engaging book, Brent R. Stockwell, a leading researcher in the exciting new science of chemical biology, describes this dilemma and the powerful techniques that may bring drug research into the twenty-first century. Filled with absorbing stories of breakthroughs, this book begins with the scientific achievements of the twentieth century that led to today's drug innovations. We learn how the invention of mustard gas in World War I led to early anti-cancer agents and how the efforts to decode the human genome might lead to new approaches in drug design. Stockwell then turns to the seemingly incurable diseases we face today, such as Alzheimer's, many cancers, and others with no truly effective medicines, and details the cellular and molecular barriers thwarting scientists equipped with only the tools of traditional pharmaceutical research. Scientists such as Stockwell are now developing methods to combat these complexities technologies for constructing and testing millions of drug candidates, sophisticated computational modeling, and entirely new classes of drug molecules all with an eye toward solving the most profound mysteries of living systems and finding cures for intractable diseases. If successful, these methods will unlock a vast terrain of untapped drug targets that could lead to a bounty of breakthrough medicines. Offering a rare, behind-the-scenes look at this cutting-edge research, The Quest for the Cure tells a thrilling story of science, persistence, and the quest to develop a new generation of cures.
Author : Richard Firn
Publisher : Oxford University Press on Demand
Page : 261 pages
File Size : 28,82 MB
Release : 2010
Category : Science
ISBN : 0199566836
This is the first monograph to describe Natural Products (NPs) as a group in an evolutionary context. It synthesizes a widely dispersed literature and provides a general picture of natural products encompassing evolution, history, ecology, and environmental issues, along with some deeper theory relevant to biochemistry.
