Privileged Scaffolds In Drug Discovery

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• Author : Stefan Bräse
• Publisher : Royal Society of Chemistry
• Release Date : 2015-11-20
• Total pages : 486
• ISBN : 9781782620303
• File Size : 17,5 Mb
• Total Download : 459
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Download Privileged Scaffolds in Medicinal Chemistry in PDF, Epub, and Kindle

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

• Author : Bin Yu,Ning Li,Caiyun Fu
• Publisher : Academic Press
• Release Date : 2023-09-01
• Total pages : 0
• ISBN : 0443186111
• File Size : 51,8 Mb
• Total Download : 202
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Download Privileged Scaffolds in Drug Discovery in PDF, Epub, and Kindle

Privileged Scaffolds in Drug Discovery is the most complete and update in the area. Covering a wide range of privileged structures, it's a perfect reference for scientists involved with targeted drug development. The editors recruited experts from several Chinese institutions to cover the areas of antiviral drugs, chalcone, pyrimidine, (benz)imidazoles, natural product derived privileged scaffolds, N-Sulfonyl carboxamides, kinase inhibitors, anti-tumor molecules, anti-neurodegenerative drugs, triazoles, oxazolidinone, indole and indoline scaffolds, tigliane diterpenoids, peptide and peptide-based drugs, quassinoids, and others including pseudo-natural products, macrocycles, stable peptides and peptidomimetics. The book will also cover 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 academy and corporate setting, investigating privileged structures to base their new drugs on. Researchers in medicinal chemistry, and chemical biology will also find the contents of the book valuable to their projects.

• Author : Larry Yet
• Publisher : John Wiley & Sons
• Release Date : 2018-03-27
• Total pages : 560
• ISBN : 9781118145661
• File Size : 10,8 Mb
• Total Download : 896
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Download Privileged Structures in Drug Discovery in PDF, Epub, and Kindle

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
• Release Date : 2015-11-20
• Total pages : 468
• ISBN : 9781782622246
• File Size : 12,5 Mb
• Total Download : 985
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Download Privileged Scaffolds in Medicinal Chemistry in PDF, Epub, and Kindle

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.

• Author : Om Silakari
• Publisher : Elsevier
• Release Date : 2018-06-11
• Total pages : 436
• ISBN : 9780081021057
• File Size : 13,8 Mb
• Total Download : 537
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Download Key Heterocycle Cores for Designing Multitargeting Molecules in PDF, Epub, and Kindle

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 : Nathan Brown
• Publisher : John Wiley & Sons
• Release Date : 2013-11-06
• Total pages : 328
• ISBN : 9783527665167
• File Size : 33,8 Mb
• Total Download : 460
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Download Scaffold Hopping in Medicinal Chemistry in PDF, Epub, and Kindle

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 : Larry Yet
• Publisher : John Wiley & Sons
• Release Date : 2018-03-07
• Total pages : 560
• ISBN : 9781118686355
• File Size : 41,7 Mb
• Total Download : 245
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Download Privileged Structures in Drug Discovery in PDF, Epub, and Kindle

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 : Victor E. Marquez
• Publisher : CRC Press
• Release Date : 2021-11-16
• Total pages : 474
• ISBN : 9781000462944
• File Size : 19,9 Mb
• Total Download : 103
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Download The Ups and Downs in Drug Design in PDF, Epub, and Kindle

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 : Andrea Basso,Seung Bum Park,Lisa Moni
• Publisher : Frontiers Media SA
• Release Date : 2019-03-22
• Total pages : 150
• ISBN : 9782889457885
• File Size : 29,9 Mb
• Total Download : 395
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Download Diversity Oriented Synthesis in PDF, Epub, and Kindle

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 : Andrea Trabocchi,Elena Lenci
• Publisher : Elsevier
• Release Date : 2019-11-23
• Total pages : 356
• ISBN : 9780128183502
• File Size : 50,9 Mb
• Total Download : 652
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Download Small Molecule Drug Discovery in PDF, Epub, and Kindle

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 : W. Andy Tao,Ying Zhang
• Publisher : John Wiley & Sons
• Release Date : 2019-07-10
• Total pages : 448
• ISBN : 9781118970218
• File Size : 25,5 Mb
• Total Download : 449
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Download Mass Spectrometry-Based Chemical Proteomics in PDF, Epub, and Kindle

PROVIDES STRATEGIES AND CONCEPTS FOR UNDERSTANDING CHEMICAL PROTEOMICS, AND ANALYZING PROTEIN FUNCTIONS, MODIFICATIONS, AND INTERACTIONS—EMPHASIZING MASS SPECTROMETRY THROUGHOUT Covering mass spectrometry for chemical proteomics, this book helps readers understand analytical strategies behind protein functions, their modifications and interactions, and applications in drug discovery. It provides a basic overview and presents concepts in chemical proteomics through three angles: Strategies, Technical Advances, and Applications. Chapters cover those many technical advances and applications in drug discovery, from target identification to validation and potential treatments. The first section of Mass Spectrometry-Based Chemical Proteomics starts by reviewing basic methods and recent advances in mass spectrometry for proteomics, including shotgun proteomics, quantitative proteomics, and data analyses. The next section covers a variety of techniques and strategies coupling chemical probes to MS-based proteomics to provide functional insights into the proteome. In the last section, it focuses on using chemical strategies to study protein post-translational modifications and high-order structures. Summarizes chemical proteomics, up-to-date concepts, analysis, and target validation Covers fundamentals and strategies, including the profiling of enzyme activities and protein-drug interactions Explains technical advances in the field and describes on shotgun proteomics, quantitative proteomics, and corresponding methods of software and database usage for proteomics Includes a wide variety of applications in drug discovery, from kinase inhibitors and intracellular drug targets to the chemoproteomics analysis of natural products Addresses an important tool in small molecule drug discovery, appealing to both academia and the pharmaceutical industry Mass Spectrometry-Based Chemical Proteomics is an excellent source of information for readers in both academia and industry in a variety of fields, including pharmaceutical sciences, drug discovery, molecular biology, bioinformatics, and analytical sciences.

• Author : M. R. Yadav,P. R. Murumkar,R. B. Ghuge
• Publisher : Elsevier
• Release Date : 2018-03-14
• Total pages : 430
• ISBN : 9780081022498
• File Size : 23,6 Mb
• Total Download : 764
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Download Vicinal Diaryl Substituted Heterocycles in PDF, Epub, and Kindle

Vicinal Diaryl-Substituted Heterocycles: A Gold Mine for the Discovery of Novel Therapeutic Agents draws together all of the key information about these compounds in one place for the first time. Following an informative overview of the importance of these structures to the discovery of potential therapeutic agents, the text goes on to outline the main compound types, with each chapter focusing on the activities of a different structure. Designed to support researchers by consolidating this important information in a single, practical guide, the authors hope to encourage further advancement and development in the discovery of novel therapeutic agents. As flexible building blocks for the production of novel compounds, vicinal diaryl-substituted heterocycles are a rich source of leads for the development of new drugs. Their adaptability means that they can be used to produce structures with a broad range of attractive characteristics, and a large number of vicinal diaryl-substituted heterocyclic compounds have already been synthesized and investigated by medicinal chemists as promising lead molecules. Collects together details of the key vicinal diaryl-substituted heterocyclic compounds in one place for the first time Highlights biological activities and SAR of derivatives Structured practically for ease of navigation between different derivatives

• Author : Girish Kumar Gupta,Vinod Kumar
• Publisher : Walter de Gruyter GmbH & Co KG
• Release Date : 2016-10-10
• Total pages : 297
• ISBN : 9783110368826
• File Size : 30,7 Mb
• Total Download : 656
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Download Chemical Drug Design in PDF, Epub, and Kindle

Chemical Drug Design provides a compact overview on recent advances in this rapidly developing field. With contributions on in silico drug design, natural product based compounds, as well as on ligand- and structure-based approaches, the authors present innovative methods and techniques for identifying and synthetically designing novel drugs.

• Author : Kunal Roy
• Publisher : Academic Press
• Release Date : 2019-02-12
• Total pages : 886
• ISBN : 9780128163771
• File Size : 30,5 Mb
• Total Download : 567
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Download In Silico Drug Design in PDF, Epub, and Kindle

In Silico Drug Design: Repurposing Techniques and Methodologies explores the application of computational tools that can be utilized for this approach. The book covers theoretical background and methodologies of chem-bioinformatic techniques and network modeling and discusses the various applied strategies to systematically retrieve, integrate and analyze datasets from diverse sources. Other topics include in silico drug design methods, computational workflows for drug repurposing, and network-based in silico screening for drug efficacy. With contributions from experts in the field and the inclusion of practical case studies, this book gives scientists, researchers and R&D professionals in the pharmaceutical industry valuable insights into drug design. Discusses the theoretical background and methodologies of useful techniques of cheminformatics and bioinformatics that can be applied for drug repurposing Offers case studies relating to the in silico modeling of FDA-approved drugs for the discovery of antifungal, anticancer, antiplatelet agents, and for drug therapies against diseases Covers tools and databases that can be utilized to facilitate in silico methods for drug repurposing

• Author : Paul A Bartlett,Michael Entzeroth
• Publisher : Royal Society of Chemistry
• Release Date : 2007-10-31
• Total pages : 444
• ISBN : 9781847552556
• File Size : 24,5 Mb
• Total Download : 177
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Download Exploiting Chemical Diversity for Drug Discovery in PDF, Epub, and Kindle

Conceptual and technological advances in chemistry and biology have transformed the drug discovery process. Evolutionary pressure among the diverse scientific and engineering disciplines that contribute to the identification of biologically active compounds has resulted in synergistic improvements at every step in the process. Exploiting Chemical Diversity for Drug Discovery encompasses the many components of this transformation and presents the current state-of-the-art of this critical endeavour. From the theoretical and operational considerations in generating a collection of compounds to screen, to the design and implementation of high-capacity and high-quality assays that provide the most useful biological information, this book provides a comprehensive overview of modern approaches to lead identification. Beginning with an introductory overview, subsequent chapters address topics that include the design of chemical libraries and methods for optimizing their diversity; automated and accelerated chemistry; high throughput assay design and detection techniques; and strategies for data analysis and property optimization. Written by experts in the field, both academic and industrial, and illustrated in full colour, this book provides an excellent overview for current practitioners and will also serve as a stimulating resource for future generations. Researchers in organic and medicinal chemistry, the biological and pharmacological sciences, as well as those interested in allied computational and engineering disciplines will value the comprehensive and up-to-date coverage.

• Author : Brent Stockwell
• Publisher : Columbia University Press
• Release Date : 2013-01-15
• Total pages : 290
• ISBN : 9780231152136
• File Size : 47,7 Mb
• Total Download : 482
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Download The Quest for the Cure in PDF, Epub, and Kindle

A leading researcher in chemical biology offers a behind-the-scenes tour of today's medical innovations, tracing key 20th-century pharmacological milestones while profiling sophisticated, emerging approaches to drug design that may enable breakthrough treatments for seemingly incurable diseases.

• Author : Anonim
• Publisher : Elsevier
• Release Date : 2017-06-03
• Total pages : 4536
• ISBN : 9780128032015
• File Size : 27,6 Mb
• Total Download : 603
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Download Comprehensive Medicinal Chemistry III in PDF, Epub, and Kindle

Comprehensive Medicinal Chemistry III provides a contemporary and forward-looking critical analysis and summary of recent developments, emerging trends, and recently identified new areas where medicinal chemistry is having an impact. The discipline of medicinal chemistry continues to evolve as it adapts to new opportunities and strives to solve new challenges. These include drug targeting, biomolecular therapeutics, development of chemical biology tools, data collection and analysis, in silico models as predictors for biological properties, identification and validation of new targets, approaches to quantify target engagement, new methods for synthesis of drug candidates such as green chemistry, development of novel scaffolds for drug discovery, and the role of regulatory agencies in drug discovery. Reviews the strategies, technologies, principles, and applications of modern medicinal chemistry Provides a global and current perspective of today's drug discovery process and discusses the major therapeutic classes and targets Includes a unique collection of case studies and personal assays reviewing the discovery and development of key drugs

• Author : Aleksey Kuznetsov
• Publisher : BoD – Books on Demand
• Release Date : 2021-06-30
• Total pages : 148
• ISBN : 9781839681790
• File Size : 27,7 Mb
• Total Download : 468
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Download Azoles in PDF, Epub, and Kindle

Azoles are a broad and promising class of five-membered heterocyclic compounds containing from one up to five nitrogen atom(s) that can also contain sulfur or oxygen atoms. Widely used as potent antifungal agents, various azole derivatives have also demonstrated many other promising biological properties. This book covers studies of several types of thiazole-based heterocyclic scaffolds, the development of 4-thiazolidinone and thiazole derivatives with heterocyclic fragments as potential candidates for new drugs against trypanosomiasis, numerous synthetic approaches for the synthesis of 1,2,3-triazoles, the application of N-azole, N,S-azole, and N,O-azole as well as their derivatives as retarders of metallic corrosion, and the integration of azoles in materials used for renewable energy processing and applications and wood treatment.

• Author : Vinod K. Tiwari
• Publisher : Elsevier
• Release Date : 2020-07-31
• Total pages : 714
• ISBN : 9780128166765
• File Size : 39,8 Mb
• Total Download : 481
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Download Carbohydrates in Drug Discovery and Development in PDF, Epub, and Kindle

Carbohydrates in Drug Discovery and Development: Synthesis and Applications examines recent and notable developments in the synthesis, biology, therapeutic, and biomedical applications of carbohydrates, which is considered to be a highly promising area of research in the field of medicinal chemistry. Their role in several important biological processes, notably energy storage, transport, modulation of protein function, intercellular adhesion, malignant transformation, signal transduction, viral, and bacterial cell surface recognition formulate the carbohydrate systems to be an exceedingly considerable scaffold for the development of new chemical entities of pharmacological importance. In addition to their easy accessibility, high functionality and chiralpool characteristics are the few additional fascinating structural features of carbohydrates, which further enhance their utilities and thus they have been able to attract chemists and biologists toward harnessing these properties for the past several decades. This book covers an advanced aspect of carbohydrate-based molecular scaffolding, starting with a general introduction followed by a detailed discussion about the impact of diverse carbohydrate-containing molecules of great therapeutic values and their impact on drug discovery and development. The topics covered in this book include the significance of heparin mimetics as the possible tools for the modulation of biology and therapy, chemistry and bioactivities of C-glycosylated compounds, inositols, iminosugars, KDO, sialic acids, glycohybrids, macrocycles, plant oligosaccharides, anti-bacterial and anti-cancer vaccines, antibiotics, and more. • Presents a practical and detailed overview of a wide range of carbohydrate systems including KDO, sialic acids, inositols, iminosugars, etc relevant for drug discovery and development. • Highlights the use of functionalized carbohydrates as synthons for the construction of various systems. • Covers recent developments in the synthesis of various glycohybrid molecules and vaccines. • Highlights the significance of heparin mimetics as tools for the modulation of biology. • Provides an impact of glycan microarrays and carbohydrate– protein interaction.

• Author : Vincent J. Merluzzi,Julian Adams
• Publisher : Springer Science & Business Media
• Release Date : 2012-12-06
• Total pages : 304
• ISBN : 9781461598466
• File Size : 29,8 Mb
• Total Download : 866
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Download The Search for Anti-Inflammatory Drugs in PDF, Epub, and Kindle

Perspectives on Anti-Inflammatory Drugs Inflammation is a very complicated process of interrelated events and cas cades that does not allow for an easily defined, focused attack for drug discovery. It is evident from years of research and development that certain classes of compounds (e.g., NSAIDs, steroids, and so on) have had a meas ure of success in alleviating pain and even dampening cellularlhormonal mechanisms involved in the process. Clear, mechanism-related therapies (e.g., for arthritis) and targeted drugs (e.g., for transplantation) have not been available in the past and, in reality, research in inflammation has re lied on more phenomenological approaches for resolving symptoms or on blatant cytoreductive approaches in cases like organ transplantation. In the last decade, approaches that have revealed novel cellular pathways in which intervention is possible for lymphocyte regulation (for example, cyclosporine and FK506) and small molecular weight mediators (e.g., leu kotriene inhibitors) are now either standard therapy or will be in a short time. These latter approaches have been the result of research from the 1970s up to the present.

• Author : Brian M. Day
• Publisher : Unknown
• Release Date : 2022
• Total pages : 0
• ISBN : OCLC:1371267212
• File Size : 40,6 Mb
• Total Download : 147
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Download OXAZOLIDINONES AS A PRIVILEGED SCAFFOLD AND PRELIMINARY EVALUATION in PDF, Epub, and Kindle

Drug discovery contains many strategies, one of which is the privileged scaffold strategy. This strategy incorporates a similar molecular framework within a collection of drug-like compounds in order to target various receptors. These scaffolds are useful to drug discovery scientists since they assist in developing libraries as well as demonstrating selectivity to a target. Oxazolidinones are 5-membered heterocyclic compound containing an oxygen, a nitrogen, and a carbonyl within the ring system. In this present study, the oxazolidinone structure was utilized as a privileged scaffold to target serotonin receptor 7 (5-HT7), mutated BRAF kinase (BRAFV6000E), Bruton's tyrosine kinase (BTK), and Cyclin-dependent protein kinase 4 and 6 (CDK4/6). Aryl piperazines and piperidines were integrated as another privileged scaffold to support the selectivity towards 5-HT7, while aminopyrimidines were employed to increase binding against the kinases. The 5-HT7 oxazolidinone series was successfully synthesized and analyzed against 5-HT7; however, the three kinase oxazolidinone series were not successfully synthesized.Candidemia is the most common bloodstream infection in the U.S. and is associated with high patient mortality rates. Due to prolonged and/or repeated clinical use of current antifungal agents, drug-resistant fungi have become an emerging problem. There is a need for new antifungals to assist in overcoming drug resistant fungi. In the second project outlined in this work, a series of ketoconazole analogs were designed and successfully synthesized. The ketoconazole analogs exhibited antifungal activity; however, no clear trends were observed in this series. Overall, the series exhibited less CYP3A4 inhibition than the parent compound, ketoconazole.