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The extraordinary potential of fluorine-containing molecules in medicinal chemistry and chemical biology has been recognized by researchers outside of the traditional fluorine chemistry field, and thus a new wave of fluorine chemistry is rapidly expanding its biomedical frontiers. With several of the best selling drugs in the world crucially containing fluorine atoms, the incorporation of fluorine to drug leads has become an essential practice in biomedical research, especially for drug design and discovery as well as development. Focusing on the unique and significant roles that fluorine plays in medicinal chemistry and chemical biology, this book reviews recent advances and future prospects in this rapidly developing field. Topics covered include: Discovery and development of fluorine containing drugs and drug candidates. New and efficient synthetic methods for medicinal chemistry and the optimisation of fluorine-containing drug candidates. Structural and chemical biology of fluorinated amino acids and peptides. Fluorine labels as probes in metabolic study, protein engineering and clinical diagnosis. Applications of 19F NMR spectroscopy in biomedical research. An appendix presents an invaluable index of all fluorine-containing drugs that have been approved by the US Food and Drug Administration, including information on structure and pharmaceutical action. Fluorine in Medicinal Chemistry and Chemical Biology will serve as an excellent reference source for graduate students as well as academic and industrial researchers who want to take advantage of fluorine in biomedical research.
Fluorine chemistry is an expanding area of research that is attracting international interest, due to the impact of fluorine in drug discovery and in clinical and molecular imaging (e.g. PET, MRI). Many researchers and academics are entering this area of research, while scientists in industrial and clinical environments are also indirectly exposed to fluorine chemistry through the use of fluorinated compounds for imaging.This book provides an overview of the impact that fluorine has made in the life sciences. In the first section, the emphasis is on how fluorine substitution of amino acids, peptides, nucleobases and carbohydrates can provide invaluable information at a molecular level. The following chapters provide answers to the key questions posed on the importance of fluorine in drug discovery and clinical applications. For examples, the reader will discover how fluorine has found its place as a key element improving drug efficacy, with reference to some of the best-selling drugs on the market. Finally, a thorough review on the design, synthesis and use of 18F-radiotracers for positron emission tomography is provided, and this is complemented with a discussion on how 19F NMR has advanced molecular and clinical imaging./a
Provides a thorough overview of the role of fluorine in pharmaceutical science and development Includes chapters on fluorinated analogues of natural products, fluorinated amino acids and peptides, and derivatives of sugars Classifies marketed and in-development fluorinated pharmaceuticals according to their therapeutic classes
Organofluorine Compounds in Biology and Medicine covers topics on biochemically relevant organofluorine compounds and their synthesis and biochemical pathways. Organofluorine compounds have renewed interest in pharmaceutical industry, and therefore a concise book on this topic is highly relevant to the scientific community involved in this area. - Covers the synthesis, biochemical, and therapeutic applications of organofluorine compounds - Offers a complete text on biochemically relevant organofluorine compounds and their synthesis and mechanistic pathways - Provides one of the first major reference books on the biological and medicinal applications of organofluorine chemistry
Fluorine in Life Sciences: Pharmaceuticals, Medicinal Diagnostics and Agrochemicals, volume four in Alain Tressaud's Progress in Fluorine Science series, presents a critical, multidisciplinary overview of the contributions of fluorinated products to solve important global issues in various life science fields, particularly in medicinal chemistry, molecular imaging techniques and agriculture. Edited by recognized experts, this book provides unique coverage of the wide-ranging uses and implications of fluorine and fluorinated compounds. Topics include medicinal monitoring and diagnosis, 19F MRI in medicine and in vivo cell tracking, 18F-labeled radiopharmaceuticals, brain imaging and neurology, risk assessment of reactive metabolites in drug discovery, and more. Edited by Alain Tressaud, past Chair and founder of the CNRS French Fluorine Network, each book in the collection also includes the work of highly-respected volume editors and contributors from both academia and industry who bring valuable and varied content to this active field. - Covers a wide range of topics - from organic and physical chemistry, to pharmaceuticals, agrochemicals and medical diagnostics - Describes major modern syntheses and unique reaction mechanisms yielding fluorine compounds in these diverse life science settings - Features contributions from a wealth of global experts - Acts as the fourth volume in Alain Tressaud's Progress in Fluorine Science
This book focuses on the new frontiers of organofluorine chemistry in synthetic, organometallic, bioorganic, medicinal, agricultural, and materials chemistry as well as chemical physics and their applications to biomedical and material sciences. The extraordinary potential of fluorine-containing molecules in biology, pharmaceuticals, agrochemical, materials and their wide range of applications has been recognized by researchers who are not in the traditional fluorine chemistry field, and thus the new wave of organofluorine chemistry is rapidly expanding its frontiers.Featuring major leading researchers from all over the world and their cutting-edge research projects, this title reviews the recent advances and envision the new exciting developments in the future. Frontiers of Organofluorine Chemistry is an excellent reference book for professional researchers, and graduate students, in both industry and academia to get inspirations and new ideas for their projects.
This first overview of mass spectrometry-based pharmaceutical analysis is the key to improved high-throughput drug screening, rational drug design and analysis of multiple ligand-target interactions. The ready reference opens with a general introduction to the use of mass spectrometry in pharmaceutical screening, followed by a detailed description of recently developed analytical systems for use in the pharmaceutical laboratory. Applications range from simple binding assays to complex screens of biological activity and systems containing multiple targets or ligands -- all highly relevant techniques in the early stages in drug discovery, from target characterization to hit and lead finding.
Late-Stage Fluorination of Bioactive Molecules and Biologically-Relevant Substrates reviews how the use of these techniques on compounds with already known and relevant biological activity can provide new pharmaceutical leads with improved medicinal properties. The fluorination strategies discussed take into account both conventional and novel reagents, including nucleophilic, electrophilic, those of a radical nature, and diverse families of organic compounds, such as (hetero) aromatic rings and aliphatic substrates. Drawing on the authors' expert knowledge, this book provides researchers with a broad set of applicable methods to use in their work.
Written with the practicing medicinal chemist in mind, this is the first modern handbook to systematically address the topic of bioisosterism. As such, it provides a ready reference on the principles and methods of bioisosteric replacement as a key tool in preclinical drug development. The first part provides an overview of bioisosterism, classical bioisosteres and typical molecular interactions that need to be considered, while the second part describes a number of molecular databases as sources of bioisosteric identification and rationalization. The third part covers the four key methodologies for bioisostere identification and replacement: physicochemical properties, topology, shape, and overlays of protein-ligand crystal structures. In the final part, several real-world examples of bioisosterism in drug discovery projects are discussed. With its detailed descriptions of databases, methods and real-life case studies, this is tailor-made for busy industrial researchers with little time for reading, while remaining easily accessible to novice drug developers due to its systematic structure and introductory section.
Essentials of Organic Chemistry is an accessible introduction to the subject for students of Pharmacy, Medicinal Chemistry and Biological Chemistry. Designed to provide a thorough grounding in fundamental chemical principles, the book focuses on key elements of organic chemistry and carefully chosen material is illustrated with the extensive use of pharmaceutical and biochemical examples. In order to establish links and similarities the book places prominence on principles and deductive reasoning with cross-referencing. This informal text also places the main emphasis on understanding and predicting reactivity rather than synthetic methodology as well as utilising a mechanism based layout and featuring annotated schemes to reduce the need for textual explanations. * tailored specifically to the needs of students of Pharmacy Medical Chemistry and Biological Chemistry * numerous pharmaceutical and biochemical examples * mechanism based layout * focus on principles and deductive reasoning This will be an invaluable reference for students of Pharmacy Medicinal and Biological Chemistry.