Privileged Scaffolds In Medicinal Chemistry


Privileged Scaffolds In Medicinal Chemistry
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Privileged Scaffolds In Medicinal Chemistry


Privileged Scaffolds In Medicinal Chemistry
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Author : Stefan Bräse
language : en
Publisher: Royal Society of Chemistry
Release Date : 2015-11-20

Privileged Scaffolds In Medicinal Chemistry written by Stefan Bräse and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-11-20 with Medical categories.


This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.



Privileged Structures In Drug Discovery


Privileged Structures In Drug Discovery
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Author : Larry Yet
language : en
Publisher:
Release Date : 2018

Privileged Structures In Drug Discovery written by Larry Yet and has been published by this book supported file pdf, txt, epub, kindle and other format this book has been release on 2018 with MEDICAL categories.


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.



Privileged Scaffolds In Drug Discovery


Privileged Scaffolds In Drug Discovery
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Author : Bin Yu
language : en
Publisher: Elsevier
Release Date : 2023-07-19

Privileged Scaffolds In Drug Discovery written by Bin Yu and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2023-07-19 with Medical categories.


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



Drug Discovery With Privileged Building Blocks


Drug Discovery With Privileged Building Blocks
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Author : Jie Jack Li
language : en
Publisher: CRC Press
Release Date : 2021-10-21

Drug Discovery With Privileged Building Blocks written by Jie Jack Li and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-10-21 with Medical categories.


Drug Discovery with Privileged Building Blocks traces back PharmaBlock’s founding philosophy of designing privileged building blocks. High-quality building blocks are crucial not only to biological activities of different molecules but also to ADMET properties, which eventually will impact the success rate of drug discovery projects. A thorough study of how building blocks perform in drug molecules and a regular analysis of new building block structures in the latest researches have proven to be a fruitful strategy to generate novel building blocks. Using this strategy, PharmaBlock has supplied the drug industry with a great number of building blocks, which are increasingly being adopted by drug hunters, and these are identified in this book. Each chapter may be read and studied without learning the previous chapters. This book will be a good starting point for novice medicinal chemists, and veteran medicinal chemists will find it useful as well. Key Feature The book covers privileged building blocks appearing most frequently on patents for novel drugs. The latest relevant tactics are explained in the context of drug design and medicinal chemistry. Key synthesis, especially large-scale synthesis, is described. The most recent literature references are cited.



Scaffold Hopping In Medicinal Chemistry


Scaffold Hopping In Medicinal Chemistry
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Author : Nathan Brown
language : en
Publisher: John Wiley & Sons
Release Date : 2013-11-06

Scaffold Hopping In Medicinal Chemistry written by Nathan Brown and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2013-11-06 with Medical categories.


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.



Privileged Scaffolds In Medicinal Chemistry


Privileged Scaffolds In Medicinal Chemistry
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Author : Stefan Bräse
language : en
Publisher: Royal Society of Chemistry
Release Date : 2015-11-20

Privileged Scaffolds In Medicinal Chemistry written by Stefan Bräse and has been published by Royal Society of Chemistry this book supported file pdf, txt, epub, kindle and other format this book has been release on 2015-11-20 with Medical categories.


One strategy to expedite the discovery of new drugs, a process that is somewhat slow and serendipitous, is the identification and use of privileged scaffolds. This book covers the history of the discovery and use of privileged scaffolds and addresses the various classes of these important molecular fragments. The first of the benzodiazepines, a class of drugs that is powerful for treating anxiety, may not have been discovered had it not been for a chance experiment on the contents of a discarded flask found during a lab clean-up. Some years later, scientists discovered that benzodiazepine derivatives were also effective in treating other diseases. This class of molecules was the first to be described as privileged in the sense that it is especially effective at altering the course of disease. Other privileged molecular structures have since been discovered, and since these compounds are so effective at interacting with numerous classes of proteins, they may be an effective starting point to look for new drugs against the supposedly “undruggable” proteins. Following introductory chapters presenting an overview, a historical perspective and the theoretical background and findings, main chapters describe the structure of privileged structures in turn and discuss major drug classes associated with them and their syntheses. This book provides comprehensive coverage of the subject through chapters contributed by expert authors from both academia and industry and will be an excellent reference source for medicinal chemists of a range of disciplines and experiences.



Recent Advances In The Synthesis Functionalization And Applications Of Pyrazole


Recent Advances In The Synthesis Functionalization And Applications Of Pyrazole
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Author : Artur M. S Silva
language : en
Publisher: Mdpi AG
Release Date : 2022-10-11

Recent Advances In The Synthesis Functionalization And Applications Of Pyrazole written by Artur M. S Silva and has been published by Mdpi AG this book supported file pdf, txt, epub, kindle and other format this book has been release on 2022-10-11 with Science categories.


Pyrazoles and their reduced form, pyrazolines, are considered privileged scaffolds in medicinal chemistry, owing to their noteworthy biological activities, physicochemical properties and occurrence in many low-molecular-weight compounds present in several marketed drugs (e.g., Celebrex(R) and Viagra(R)). Pyrazoles are also found in a variety of agrochemicals (fungicides, insecticides, and herbicides) and are versatile compounds for synthetic manipulations. Their challenging chemical structures and properties (mainly tautomerism, with possible implications in their reactivity), and diverse applications, have attracted the attention of many researchers who have developed various synthetic approaches. This reprint presents some examples of the most recent advances in pyrazoles' chemistry, including synthetic methodologies to access novel pyrazole derivatives, to their functionalization, and studies of their properties and applications in different fields, mainly in medicine and materials science.



The Ups And Downs In Drug Design


The Ups And Downs In Drug Design
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Author : Victor E. Marquez
language : en
Publisher: CRC Press
Release Date : 2021-11-15

The Ups And Downs In Drug Design written by Victor E. Marquez and has been published by CRC Press this book supported file pdf, txt, epub, kindle and other format this book has been release on 2021-11-15 with Medical categories.


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



Peptidomimetics In Organic And Medicinal Chemistry


Peptidomimetics In Organic And Medicinal Chemistry
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Author : Antonio Guarna
language : en
Publisher: John Wiley & Sons
Release Date : 2014-04-07

Peptidomimetics In Organic And Medicinal Chemistry written by Antonio Guarna and has been published by John Wiley & Sons this book supported file pdf, txt, epub, kindle and other format this book has been release on 2014-04-07 with Science categories.


A peptidomimetic is a small protein-like chain designed to mimic a peptide with adjusted molecular properties such as enhanced stability or biological activity. It is a very powerful approach for the generation of small-molecule-based drugs as enzyme inhibitors or receptor ligands. Peptidomimetics in Organic and Medicinal Chemistry outlines the concepts and synthetic strategies underlying the building of bioactive compounds of a peptidomimetic nature. Topics covered include the chemistry of unnatural amino acids, peptide- and scaffold-based peptidomimetics, amino acid-side chain isosteres, backbone isosteres, dipeptide isosteres, beta-turn peptidomimetics, proline-mimetics as turn inducers, cyclic scaffolds, amino acid surrogates, and scaffolds for combinatorial chemistry of peptidomimetics. Case studies in the hit-to-lead process, such as the development of integrin ligands and thrombin inhibitors, illustrate the successful application of peptidomimetics in drug discovery.



Small Molecule Drug Discovery


Small Molecule Drug Discovery
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Author : Andrea Trabocchi
language : en
Publisher: Elsevier
Release Date : 2019-11-23

Small Molecule Drug Discovery written by Andrea Trabocchi and has been published by Elsevier this book supported file pdf, txt, epub, kindle and other format this book has been release on 2019-11-23 with Science categories.


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