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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
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.
In view of increasing interest in organofluorine compounds, this book was undertaken to describe biological and physical properties of organofluorine compounds, synthetic methods of these, their roles in pharmaceutical, agrochemical and material sciences. In particular, the book will emphasize on the usefulness of fluorination reaction, availability of fluorination agents, so that even graduate students who are unfamiliar to this field can understand and participate in this fascinating heteroatom chemistry.
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.
Emphasizing structure, scope, and synthesis, as well as synthesis planning and methodology, it covers a wide variety of biologically active fluorine-containing compounds. A biological rationale is given for the design and biological fate of the described molecules.
Fluorine and Health presents a critical multidisciplinary overview on the contribution of fluorinated compounds to resolve the important global issue of medicinal monitoring and health care. The involved subjects are organized in three thematic parts devoted to Molecular Imaging, Biomedical Materials and Pharmaceuticals. Initially the key-position of partially fluorinated low molecular weight compounds labelled either with the natural 19F-isotope for Magnetic Resonance Imaging (MRI) or labelled with the radioactive [18F]-isotope for Positron Emission Tomography (PET) is highlighted. Both non-invasive methods belong to the most challenging in vivo imaging techniques in oncology, neurology and in cardiology for the diagnosis of diseases having the highest mortality in the industrialized countries. The manifold facets of fluorinated biomaterials range from inorganic ceramics to perfluorinated organic molecules. Liquid perfluorocarbons are suitable for oxygen transport and as potential respiratory gas carriers, while fluorinated polymers are connected to the pathology of blood vessels. Another important issue concerns the application of highly fluorinated liquids in ophthalmology. Moreover, fluorine is an essential trace element in bone mineral, dentine and tooth enamel and is applied for the prophylaxis and treatment of dental caries. The various origins of human exposure to fluoride species is detailed to promote a better understanding of the effect of fluoride species on living organisms.Medicinally relevant fluorinated molecules and their interactions with native proteins are the main focus of the third part. New molecules fluorinated in strategic position are crucial for the development of pharmaceuticals with desired action and optimal pharmacological profile. Among the hundreds of marketed active drug components there are more than 150 fluorinated compounds. The chapters will illustrate how the presence of fluorine atoms alters properties of bioactive compounds at various biochemical steps, and possibly facilitate its emergence as pharmaceuticals. Finally the synthetic potential of a fluorinase, the first C-F bond forming enzyme, is summarized. - New approach of topics involving chemistry, biology and medicinal techniques - Transdisciplinar papers on fluoride products - Importance of fluoride products in health - Updated data on specific topics
Following its well-received predecessor, this book offers an essential guide to chemists for understanding fluorine in spectroscopy. With over 1000 compounds and 100 spectra, the second edition adds new data – featuring fluorine effects on nitrogen NMR, chemical shifts, and coupling constants. • Explains how to successfully incorporate fluorine into target molecules and utilize fluorine substituents to structurally characterize organic compounds • Includes new data on nitrogen NMR, focusing on N-15, to portray the influence of fluorine upon nitrogen NMR chemical shifts and coupling constants • Expands on each chapter from the first edition with additional data and updated discussion from recent findings • "The flawless ordering of material covered in this stand-alone volume is such that information can be found very easily." – Angewandte Chemie review of the first edition, 2010
In recent years, organo-fluorine chemistry has made a marked impact on the design and synthesis of a large variety of biologically active molecules, such as steroids, carbohydrates, amines, amino acids, peptides and other natural products. Naturally occurring amino acids play a pivotal role in living systems, and therefore synthetic fluorine-containing amino acids have been of significant interest to researchers working towards the understanding and modification of physiological processes. Fluorine-containing Amino Acids: is the first volume devoted to the synthesis and properties of fluorine-containing amino acids pays special attention to the preparation of enantiomerically pure acids (which are essential to the modern pharmaceutical industry) deals with a rapidly expanding field of research has been written by experienced researchers who are responsible for many developments in the field highlights the interdisciplinary nature of this topic Fluorine-containing Amino Acids is the only dedicated reference in this subject and will be essential for researchers in synthetic organic, peptide, natural product, and medicinal chemistry and biochemistry.
This is a fascinating introduction to the topic. Spanning the spectrum of nucleic acid chemistry, carbohydrates, peptides, molecular recognition, biosynthesis and natural biosynthesis, right up to medical and biophysical chemistry, the book provides advanced students and those already working in the field with a balanced overview. In more than 30 contributions, a new generation of recognized scientists gives an account of the latest research in such areas as * Artificial receptors for the stabilization of ß-sheet structures * Carbohydrate recognition by artificial receptors * Combinatorial chemistry as a tool for the discovery of catalysts * The interaction of NO and peroxynitrite with hemoglobin and myoglobin * Inhibitors against human mast-cell-tryptase as a potential approach to conquering asthma * The selectivity of DNA replication. A readily accessible survey for everyone wishing to stay abreast of developments. With a Foreword by Ronald Breslow.
Modern Synthesis Processes and Reactivity of Fluorinated Compounds focuses on the exceptional character of fluorine and fluorinated compounds. This comprehensive work explores examples taken from all classes of fluorine chemistry and illustrates the extreme reactivity of fluorinating media and the peculiar synthesis routes to fluorinated materials. The book provides advanced and updated information on the latest synthesis routes to fluorocompounds and the involved reaction mechanisms. Special attention is given to the unique reactivity of fluorine and fluorinated media, along with the correlation of those properties to valuable applications of fluorinated compounds. - Contains quality content edited, and contributed, by leading scholars in the field - Presents applied guidance on the preparation of original fluorinated compounds, potentially transferable from the lab scale to industrial applications - Provides practical synthesis information for a wide audience interested in fluorine compounds in many branches of chemistry, materials science, and physics