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This book describes cutting-edge organic syntheses of biologically active compounds, isolation of pharmaceutically promising compounds from microorganisms, drug design, and progress on chemical biology. Synthetic strategy and tactics are summarized for super-carbon chain compounds, antitumor polycycles, aryl C-glycoside, antimycins, duocarmycins, cannabinoids, and other compounds. Special chapters are devoted to synthesis and biochemistry of fatty acid metabolites, which play a central role in the initiation and resolution of inflammation. The book provides a quick survey of trending topics in organic synthesis and chemical tools for biological investigation, and furnishes ideas for future research in organic synthesis. In addition, the contents can easily be understood by young chemists, graduate students, and those who are looking for new research based on organic chemistry.
Studies in Natural Products Chemistry, Volume 73 covers the synthesis, testing and recording of medicinal properties of natural products, providing cutting-edge accounts of fascinating developments in the isolation, structure elucidation, synthesis, biosynthesis and pharmacology of a diverse array of bioactive natural products. Natural products in the plant and animal kingdom offer a huge diversity of chemical structures that are the result of biosynthetic processes that have been modulated over millennia through genetic effects. With rapid developments in spectroscopic techniques and accompanying advances in high-throughput screening techniques, it has become possible to isolate and determine the structures and biological activity of natural products. Hence, these new discoveries have created new avenues and applications for their use. - Focuses on the chemistry of bioactive natural products - Contains contributions by leading authorities in the field - Presents sources of new pharmacophores
Total Synthesis of Bioactive Natural Products provides step-by-step guidelines for effectively synthesizing the most promising bioactive agents from a broad range of natural products. Beginning with a concise background that outlines the benefits and challenges faced in effective synthesis, the book goes on to provide individual outlines for approximately 100 of the most promising bioactive agents. Taking a logical, user-friendly approach, the systematic name, compound class, structure, natural source, pharmaceutical potential and synthetic routes for each structure are detailed, with clear illustrations throughout, making this book an essential and practical guide for anyone working with both synthesis and natural products. - Provides individual outlines for the total synthesis of approximately 100 bioactive natural molecules - Outlines each step of the process in detail, with full experimental information supported by extensive schemes - Includes retrosynthetic analyses, reaction sequences and stereochemically crucial steps for each molecule
During the last decade, national and international scientific organizations have become increasingly engaged in considering how to respond to the biosecurity implications of developments in the life sciences and in assessing trends in science and technology (S&T) relevant to biological and chemical weapons nonproliferation. The latest example is an international workshop, Trends in Science and Technology Relevant to the Biological Weapons Convention, held October 31 - November 3, 2010 at the Institute of Biophysics of the Chinese Academy of Sciences in Beijing. Life Sciences and Related Fields summarizes the workshop, plenary, and breakout discussion sessions held during this convention. Given the immense diversity of current research and development, the report is only able to provide an overview of the areas of science and technology the committee believes are potentially relevant to the future of the Biological and Toxic Weapons Convention (BWC), although there is an effort to identify areas that seemed particularly ripe for further exploration and analysis. The report offers findings and conclusions organized around three fundamental and frequently cited trends in S&T that affect the scope and operation of the convention: The rapid pace of change in the life sciences and related fields; The increasing diffusion of life sciences research capacity and its applications, both internationally and beyond traditional research institutions; and The extent to which additional scientific and technical disciplines beyond biology are increasingly involved in life sciences research. The report does not make recommendations about policy options to respond to the implications of the identified trends. The choice of such responses rests with the 164 States Parties to the Convention, who must take into account multiple factors beyond the project's focus on the state of the science.
Discovery and Development of Antidiabetic Agents from Natural Products brings together global research on the medicinal chemistry of active agents from natural sources for the prevention and treatment of diabetes and associated disorders. From the identification of promising leads, to the extraction and synthesis of bioactive molecules, this book explores a range of important topics to support chemists in the discovery and development of safer, more economical therapeutics that are desperately needed in response to this emerging global epidemic. Beginning with an overview of bioactive chemical compounds from plants with anti-diabetic properties, the book goes on to outline the identification and extraction of anti-diabetic agents and antioxidants from natural sources. It then explores anti-diabetic plants from specific regions before looking more closely at the background, isolation, and synthesis of key therapeutic compounds and their derivatives, including Mangiferin, Resveratrol, natural saponins, and alpha-glucosidase enzyme inhibitors. The book concludes with a consideration of current and potential future applications. Combining the expertise of specialists from around the world, this volume aims to support and encourage medicinal chemists investigating natural sources as starting points for the development of standardized, safe, and effective antidiabetic therapeutics. - Contains chapters written by active researchers and leading global experts who are deeply engaged in the research field of natural product chemistry for drug discovery - Provides comprehensive coverage of cutting-edge research advances in the design of medicinal natural products with potential as preventives and therapeutics for diabetes and related metabolic issues - Presents a practical review of the identification, isolation, and extraction techniques that help support medicinal chemists in the lab
Natural compounds, which have evolved their function over millions of years, are often more efficient than man-made compounds if a specific biological activity is needed, e.g. as an enzyme inhibitor or as a toxin to kill a cancer cell. This book comprising of sixteen technical chapters, highlights the chemical and biological aspects of potential natural products with an intention of unravelling their pharmaceutical applicability in modern drug discovery processes. Key features: Covers the synthesis, semi-synthesis and also biosynthesis of potentially bioactive natural products Features chemical and biological advances in naturally occurring organic compounds describing their chemical transformations, mode of actions, and structure-activity relationships 40 expert scientists from around the world report their latest findings and outline future opportunities for the development of novel and highly potent drugs based on natural products operating at the interface of chemistry and biology Forward-looking: Addresses opportunities and cutting-edge developments rather than well-documented basic knowledge, pinpoints current trends and future directions in this rapidly-evolving field Application-oriented: Throughout the book, the focus is on actual and potential applications in pharmacology and biotechnology This book is an essential resource for natural products chemists, medicinal chemists, biotechnologists, biochemists, pharmacologists, as well as the pharmaceutical and biotechnological industries.
Discover an enhanced synthetic approach to developing and screening chemical compound libraries Diversity-oriented synthesis is a new paradigm for developing large collections of structurally diverse small molecules as probes to investigate biological pathways. This book presents the most effective methods in diversity-oriented synthesis for creating small molecule collections. It offers tested and proven strategies for developing diversity-oriented synthetic libraries and screening methods for identifying ligands. Lastly, it explores some promising new applications based on diversity-oriented synthesis that have the potential to dramatically advance studies in drug discovery and chemical biology. Diversity-Oriented Synthesis begins with an introductory chapter that explores the basics, including a discussion of the relationship between diversity-oriented synthesis and classic combinatorial chemistry. Divided into four parts, the book: Offers key chemical methods for the generation of small molecules using diversity-oriented principles, including peptidomimetics and macrocycles Expands on the concept of diversity-oriented synthesis by describing chemical libraries Provides modern approaches to screening diversity-oriented synthetic libraries, including high-throughput and high-content screening, small molecule microarrays, and smart screening assays Presents the applications of diversity-oriented synthetic libraries and small molecules in drug discovery and chemical biology, reporting the results of key studies and forecasting the role of diversity-oriented synthesis in future biomedical research This book has been written and edited by leading international experts in organic synthesis and its applications. Their contributions are based on a thorough review of the current literature as well as their own firsthand experience developing synthetic methods and applications. Clearly written and extensively referenced, Diversity-Oriented Synthesis introduces novices to this highly promising field of research and serves as a springboard for experts to advance their own research studies and develop new applications.
Drug design is a complex, challenging and innovative research area. Structure-based molecular design has transformed the drug discovery approach in modern medicine. Traditionally, focus has been placed on computational, structural or synthetic methods only in isolation. This one-of-akind guide integrates all three skill sets for a complete picture of contemporary structure-based design. This practical approach provides the tools to develop a high-affinity ligand with drug-like properties for a given drug target for which a high-resolution structure exists. The authors use numerous examples of recently developed drugs to present "best practice" methods in structurebased drug design with both newcomers and practicing researchers in mind. By way of a carefully balanced mix of theoretical background and case studies from medicinal chemistry applications, readers will quickly and efficiently master the basic skills of successful drug design. This book is aimed at new and active medicinal chemists, biochemists, pharmacologists, natural product chemists and those working in drug discovery in the pharmaceutical industry. It is highly recommended as a desk reference to guide students in medicinal and chemical sciences as well as to aid researchers engaged in drug design today.
These proceedings gather carefully selected, peer-reviewed contributions from the International Conference on Pure and Applied Chemistry (ICPAC 2018). The event, the latest installment in a biennial conference series, was held in July 2018 in Mauritius. The respective chapters in this unique collection reflect a wide range of fundamental and applied research in the chemical sciences and various interdisciplinary subjects. In addition to reviews, they highlight cutting-edge advances.