Download or read book Synthesis and Structure Activity Relationship Studies of a Natural Product derived Compound Library written by Paul Whitney Swain and published by . This book was released on 2010 with total page 351 pages. Available in PDF, EPUB and Kindle. Book excerpt: Infectious diseases will always be a public health concern. The incidence of bacterial strains found in clinical settings that exhibit resistance to our current arsenal of antimicrobial drugs has risen sharply in the past twenty years and is projected to keep rising. The Infectious Diseases Society of America (IDSA) stated that more people die of methicillin-resistant Staphylococcus aureus (MRSA) infections per year in US hospitals than HIV/AIDS and tuberculosis combined. However, stagnation of research in the area of infectious diseases over the past forty years has left us dreadfully behind in the battle against these deadly pathogens. Recently, researchers have started getting back to the roots of drug discovery by screening possible antibiotic-producing organisms isolated from the environment. Unfortunately this will take time as many of the more common antibiotics have already been found in this manner, leaving the rarest compounds to still be found. Other drug discovery programs focus on the production of large chemical libraries by combinatorial synthesis. While hundreds of thousands of compounds have been made in this way, only one FDA approved drug has been made by de novo synthesis. Compounds made by combinatorial methods lack much of the complexity afforded by natural products. Yet, it is the complexity of natural products that makes them good antibiotics. The strategy we employ is to use natural products in the synthesis of combinatorial libraries. In this manner, we are able to incorporate complexity into a large number of compounds, increasing our chances of finding a new compound with antimicrobial activity. Herein is described a compound library derived from the natural product, nonactin. A preliminary library was previously synthesized by Phillips that yielded two lead compounds that were the starting points for this work. The lead compounds were systematically modified over four iterations of a Structure Activity Relationship study in an effort to maximize antimicrobial activity. Antimicrobial activity of the compounds from the SAR study against Bacillus subtilis was increased nearly 200-fold from the initial leads and spectrum of activity was expanded to include Staphylococcus aureus and Enterococcus faecalis.

Download or read book Modern Methods of Drug Discovery written by Alexander Hillisch and published by Birkhäuser. This book was released on 2012-11-28 with total page 294 pages. Available in PDF, EPUB and Kindle. Book excerpt: Research in the pharmaceutical industry today is in many respects quite different from what it used to be only fifteen years ago. There have been dramatic changes in approaches for identifying new chemical entities with a desired biological activity. While chemical modification of existing leads was the most important approach in the 1970s and 1980s, high-throughput screening and structure-based design are now major players among a multitude of methods used in drug discov ery. Quite often, companies favor one of these relatively new approaches over the other, e.g., screening over rational design, or vice versa, but we believe that an intelligent and concerted use of several or all methods currently available to drug discovery will be more successful in the medium term. What has changed most significantly in the past few years is the time available for identifying new chemical entities. Because of the high costs of drug discovery projects, pressure for maximum success in the shortest possible time is higher than ever. In addition, the multidisciplinary character of the field is much more pronounced today than it used to be. As a consequence, researchers and project managers in the pharmaceutical industry should have a solid knowledge of the more important methods available to drug discovery, because it is the rapidly and intelligently combined use of these which will determine the success or failure of preclinical projects.

Download or read book Total Synthesis of Natural Products written by Jie Jack Li and published by Springer Science & Business Media. This book was released on 2013-03-14 with total page 292 pages. Available in PDF, EPUB and Kindle. Book excerpt: 'Total Synthesis of Natural Products' is written and edited by some of today's leaders in organic chemistry. Eleven chapters cover a range of natural products, from steroids to alkaloids. Each chapter contains an introduction to the natural product in question, descriptions of its biological and pharmacological properties and outlines of total synthesis procedures already carried out. Particular emphasis is placed on novel methodologies developed by the respective authors and their research groups. This text is ideal for graduate and advanced undergraduate students, as well as organic chemists in academia and industry.

Download or read book Combinatorial Synthesis of Natural Product Based Libraries written by Armen M. Boldi and published by CRC Press. This book was released on 2006-05-16 with total page 0 pages. Available in PDF, EPUB and Kindle. Book excerpt: Traditionally, the search for new compounds from natural products has been a time- and resource-intensive process. The recent application of combinatorial methods and high-throughput synthesis has allowed scientists to generate a range of new molecular structures from natural products and observe how they interact with biological targets. Combinatorial Synthesis of Natural Product-Based Libraries summarizes the most important perspectives on the application of combinatorial chemistry and natural products to novel drug discovery. The book details the latest approaches for implementing combinatorial research and testing methodologies to the synthesis of natural product-based libraries. Interconnecting the important aspects of this emerging field through the work of several leading scientists, it covers the computational analysis of natural molecules and details strategies for designing compound libraries, using bioinformatics in particular. The authors describe numerous synthetic methods for producing natural products and their analogs, including engineered biosynthesis and polymer-supported reagents. They also discuss additional considerations for generating libraries, such as screening, scaffolding, and yield optimization. Other chapters examine specific classes of libraries derived from natural products including carbohydrates, polyketides, peptides, alkaloids, terpenoids, steroids, flavonoids, and fungal compounds. Drawing attention to the interplay of drug discovery, natural products, and organic synthesis, Combinatorial Synthesis of Natural Product-Based Libraries contains the most recent and significant methods used to search and assess new compounds for their ability to mitigate biological processes that may lead to improved treatments for various diseases.

Download or read book 1 written by Jeffrey A. Pfefferkorn and published by . This book was released on 2000 with total page 938 pages. Available in PDF, EPUB and Kindle. Book excerpt: Biologically active natural products serve important roles in both chemistry and medicine. In this thesis, studies aimed at the solution and solid phase syntheses of several natural products and their analogs are described. First, the sarcodictyins are a collection of marine-derived diterpenoids that exhibit potent cytotoxicities against several cancer cell lines. Interestingly, these compounds function by inducing tubulin polymerization and stabilizing microtubules in a mechanism similar to that of Taxol(TM). The total syntheses of sarcodictyins A and B are presented along with a summary of the structure-activity relationships derived for this new class of anticancer agents. Second, studies towards the synthesis of garsubellin A which resulted in the construction of the fully functionalized core of this molecule are described. Interest in garsubellin A as a synthetic target resulted from its neurotrophic-like properties in several in vitro assays. Finally, preliminary efforts to achieve a solid phase synthesis of garsubellin A resulted in the development of a novel selenium based solid phase method for the synthesis of small molecule libraries. This strategy was subsequently applied to the solid phase synthesis of several benzopyran containing natural products as well as to the synthesis of a 10,000-membered discovery-oriented combinatorial library for use in chemical biology studies.

Download or read book Plant derived Natural Products written by Anne E. Osbourn and published by Springer Science & Business Media. This book was released on 2009-07-07 with total page 588 pages. Available in PDF, EPUB and Kindle. Book excerpt: Plants produce a huge array of natural products (secondary metabolites). These compounds have important ecological functions, providing protection against attack by herbivores and microbes and serving as attractants for pollinators and seed-dispersing agents. They may also contribute to competition and invasiveness by suppressing the growth of neighboring plant species (a phenomenon known as allelopathy). Humans exploit natural products as sources of drugs, flavoring agents, fragrances and for a wide range of other applications. Rapid progress has been made in recent years in understanding natural product synthesis, regulation and function and the evolution of metabolic diversity. It is timely to bring this information together with contemporary advances in chemistry, plant biology, ecology, agronomy and human health to provide a comprehensive guide to plant-derived natural products. Plant-derived natural products: synthesis, function and application provides an informative and accessible overview of the different facets of the field, ranging from an introduction to the different classes of natural products through developments in natural product chemistry and biology to ecological interactions and the significance of plant-derived natural products for humans. In the final section of the book a series of chapters on new trends covers metabolic engineering, genome-wide approaches, the metabolic consequences of genetic modification, developments in traditional medicines and nutraceuticals, natural products as leads for drug discovery and novel non-food crops.

Download or read book Combinatorial Chemistry and Molecular Diversity in Drug Discovery written by Eric M. Gordon and published by Wiley-Liss. This book was released on 1998-08-27 with total page 552 pages. Available in PDF, EPUB and Kindle. Book excerpt: COMBINATORIAL CHEMISTRY AND MOLECULAR DIVERSITY IN DRUG DISCOVERY Edited by Eric M. Gordon and James F. Kerwin, Jr. Increasing pressure to identify, optimize, develop, and commercialize novel drugs more rapidly and more cost-effectively has led to an urgent demand for technologies that can reduce the time to market for new products. Molecular diversity, of both natural and synthetic materials, provides a valuable source of compounds for identifying and optimizing new drug leads. Through the rapidly evolving technology of combinatorial chemistry, it is now possible to produce libraries of small molecules to screen for novel bioactivities. This powerful new technology has begun to help pharmaceutical companies find new drug candidates quickly, save significant dollars in preclinical development costs, and ultimately change their fundamental approach to drug discovery. Comprising the work of the leading authorities in the area of molecular diversity and combinatorial chemistry, Combinatorial Chemistry and Molecular Diversity in Drug Discovery highlights the critical concepts and issues involved in implementing combinatorial chemistry to create chemical libraries. The authors, industrial and academic experts in the field, apply combinatorial technologies to drug discovery and development and place co-evolving technologies and practices in a global framework. Included among the many topics: * Historical background. * Library strategy and design. * Solid-phase synthesis. * Small molecular libraries. * Automation, analytical, and computational methodology. * Biological diversity. * Strategies for screening combinatorial libraries. * Combinatorial drug screening and development. * Combinatorial chemistry information management. Combinatorial Chemistry and Molecular Diversity in Drug Discovery is one of the first comprehensive books to cover this explosive area. It is must reading for medicinal chemists, pharmacologists, molecular biologists, biochemists, enzymologists, and drug discovery research managers in industry, academia, and government.

Download or read book Natural Product Chemistry for Drug Discovery written by Antony D. Buss and published by Royal Society of Chemistry. This book was released on 2010 with total page 459 pages. Available in PDF, EPUB and Kindle. Book excerpt: This text provides a comprehensive summary of where natural product chemistry is today in drug discovery. It covers emerging technologies and case studies and is a source of up-to-date information on the topical subject of natural products.

Download or read book Medicinal Chemistry of Bioactive Natural Products written by Xiao-Tian Liang and published by John Wiley & Sons. This book was released on 2006-03-17 with total page 482 pages. Available in PDF, EPUB and Kindle. Book excerpt: Current discoveries and research into bioactive natural products Medicinal Chemistry of Bioactive Natural Products provides a much-needed survey of bioactive natural products and their applications in medicinal chemistry. This comprehensive reference features articles by some of the world's leading scientists in the field on discovery, structure elucidation, and elegant synthetic strategies--developed for natural products--with an emphasis on the structure activity relationship of bioactive natural products. The topics have been carefully chosen on the basis of relevance to current research and to importance as clinicially useful agents. Rather than attempting to be a comprehensive encyclopedia of bioactive natural products, Medicinal Chemistry of Bioactive Natural Products guides the reader to the key developments in the field. By providing not only practical detail but a historical perspective on the chemistry and biology of the compounds under consideration, the book serves as a handy resource for researchers in their own work developing pharmaceuticals, and as an inspiring introduction for young scientists to the dynamic field of bioactive natural products research. Enhanced by examples with updated research results, the discussion covers such topics as: * The chemistry and biology of epothilones * Vancomycin and other glycopeptide antibiotic derivates * Antitumor and other related activities of Taxol and its analogs * The antimalarial properties of the traditional Chinese medicine, Quinghaosu (artemisinin) * Huperzine A: A natural drug for the treatment of Alzheimer's disease * The medicinal chemistry of ginkgolides from Ginkgo biloba * Recent progress in Calophyllum coumarins as potent anti-HIV agents * Plant-derived anti-HIV agents and analogs * Chemical synthesis of annonaceous acetogenins and their structurally modified mimics

Download or read book Privileged Scaffolds in Medicinal Chemistry written by Stefan Bräse and published by Royal Society of Chemistry. This book was released on 2015-11-20 with total page 486 pages. Available in PDF, EPUB and Kindle. Book excerpt: This book addresses the various classes of privileged scaffolds and covers the history of their discovery and use.

Download or read book The Role of Natural Products in Drug Discovery written by J. Mulzer and published by Springer Science & Business Media. This book was released on 2013-04-17 with total page 363 pages. Available in PDF, EPUB and Kindle. Book excerpt: Natural Products have been important sources of useful drugs from prehistoric times to the present. This book gives an overview about this field and provides important recent contributions to the discovery of new drugs generated by research on natural products. Total synthesis of natural products with interesting biological activities is paving the way for the preparation of new and improved analogs. The methods of combinatorial chemistry permit the selection of the best drug from a large number of candidates. Beyond synthesis and evaluation of organic molecules a number of new bioorganic methods are coming to the fore and will be discucced in this isue of the ERnst schering Research Foundation workshop proceedings.

Download or read book Medicinal Natural Products written by Paul M. Dewick and published by John Wiley & Sons. This book was released on 2002-01-03 with total page 524 pages. Available in PDF, EPUB and Kindle. Book excerpt: This guide covers classes of natural products in medicine, whether derived from plants, micro-organisms or animals. Structured according to biosynthetic pathway, it is written from a chemistry-based approach.

Download or read book Chemistry of Biologically Potent Natural Products and Synthetic Compounds written by Shahid Ul-Islam and published by John Wiley & Sons. This book was released on 2021-06-29 with total page 434 pages. Available in PDF, EPUB and Kindle. Book excerpt: In view of their promising biological and pharmaceutical activities, natural product inspired and heterocyclic compounds have recently gained a reputation in the field of medicinal chemistry. Over the past decades, intensive research efforts have been ongoing to understand the synthesis, biochemistry and engineering involved in their preparation and action mechanisms. Several novel natural product derivatives, heterocyclic and other synthetic compounds, have been reported to have shown interesting biological activities including anticancer, antimicrobial, anti-inflammatory, anti-glycemic, anti-allergy and antiviral etc. Chemistry of Biologically Potent Natural Products and Synthetic Compounds provides up-to-date information on new developments and most recent medicinal applications of the natural products and derivatives, as well as the chemistry and synthesis of heterocyclic and other related compounds.

Download or read book Plant Bioactives and Drug Discovery written by Valdir Cechinel-Filho and published by John Wiley & Sons. This book was released on 2012-04-11 with total page 600 pages. Available in PDF, EPUB and Kindle. Book excerpt: An in-depth exploration of the applications of plant bioactive metabolites in drug research and development Highlighting the complexity and applications of plant bioactive metabolites in organic and medicinal chemistry, Plant Bioactives and Drug Discovery: Principles, Practice, and Perspectives provides an in-depth overview of the ways in which plants can inform drug research and development. An edited volume featuring multidisciplinary international contributions from acclaimed scientists researching bioactive natural products, the book provides an incisive overview of one of the most important topics in pharmaceutical studies today. With coverage of strategic methods of natural compound isolation, structural manipulation, natural products in clinical trials, quality control, and more, and featuring case studies on medicinal plants, the book serves as a definitive guide to the field of plant biodiversity as it relates to medicine. In addition, chapters on using natural products as drugs that target specific disease areas, including neurological disorders, inflammation, infectious diseases, and cancer, illustrate the myriad possibilities for therapeutic applications. Wide ranging and comprehensive, Plant Bioactives and Drug Discovery also includes important information on marketing, regulations, intellectual property rights, and academic-industry collaboration as they relate to plant-based drug research, making it an essential resource for advanced students and academic and industry professionals working in biochemical, pharmaceutical, and related fields.

Download or read book Natural Products in Medicinal Chemistry written by Stephen Hanessian and published by John Wiley & Sons. This book was released on 2013-12-18 with total page 652 pages. Available in PDF, EPUB and Kindle. Book excerpt: The inspiration provided by biologically active natural products to conceive of hybrids, congeners, analogs and unnatural variants is discussed by experts in the field in 16 highly informative chapters. Using well-documented studies over the past decade, this timely monograph demonstrates the current importance and future potential of natural products as starting points for the development of new drugs with improved properties over their progenitors. The examples are chosen so as to represent a wide range of natural products with therapeutic relevance among others, as anticancer agents, antimicrobials, antifungals, antisense nucleosides, antidiabetics, and analgesics. From the content: * Part I: Natural Products as Sources of Potential Drugs and Systematic Compound Collections * Part II: From Marketed Drugs to Designed Analogs and Clinical Candidates * Part III: Natural Products as an Incentive for Enabling Technologies * Part IV: Natural Products as Pharmacological Tools * Part V: Nature: The Provider, the Enticer, and the Healer

Download or read book Natural Products and Drug Discovery written by Subhash C. Mandal and published by Elsevier. This book was released on 2018-02-16 with total page 778 pages. Available in PDF, EPUB and Kindle. Book excerpt: Natural Products and Drug Discovery: An Integrated Approach provides an applied overview of the field, from traditional medicinal targets, to cutting-edge molecular techniques. Natural products have always been of key importance to drug discovery, but as modern techniques and technologies have allowed researchers to identify, isolate, extract and synthesize their active compounds in new ways, they are once again coming to the forefront of drug discovery. Combining the potential of traditional medicine with the refinement of modern chemical technology, the use of natural products as the basis for drugs can help in the development of more environmentally sound, economical, and effective drug discovery processes. Natural Products & Drug Discovery: An Integrated Approach reflects on the current changes in this field, giving context to the current shift and using supportive case studies to highlight the challenges and successes faced by researchers in integrating traditional medicinal sources with modern chemical technologies. It therefore acts as a useful reference to medicinal chemists, phytochemists, biochemists, pharma R&D professionals, and drug discovery students and researchers. Reviews the changing role of natural products in drug discovery, integrating traditional knowledge with modern molecular technologies Highlights the potential future role of natural products in preventative medicine Supported by real world case studies throughout

Download or read book WHO Global Report on Traditional and Complementary Medicine 2019 written by World Health Organization and published by World Health Organization. This book was released on 2019-05-16 with total page 228 pages. Available in PDF, EPUB and Kindle. Book excerpt: This report is structured in five parts: national framework for traditional and complementary medicine (T&CM); product regulation; practices and practitioners; the challenges faced by countries; and finally the country profiles. Apart from the section on practices and practitioners the report is consistent with the format of the report of the first global survey in order to provide a useful comparison. The section on practices and practitioners which covers providers education and health insurance is a new section incorporated to reflect the emerging trends in T&CM and to gather new information regarding these topics at a national level. All new information received has been incorporated into individual country profiles and data graphs. The report captures the three phases of progress made by Member States; that is before and after the first WHO Traditional Medicine Strategy (1999?2005) from the first global survey to the second global survey (2005?2012) and from the second survey to the most recent timeline (2012?2018).