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.
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
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.
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.
This two-volume work combines comprehensive information on the chemistry of the fluorinated heterocycles. The material has been divided such that the first volume is dedicated to 5-membered fluorinated heterocycles and macrocycles, while the second volume combines data connected with the chemistry of fluorine containing 6-membered heterocycles. Both volumes will be of interest to synthetic organic chemists in general, and particularly for those colleagues working in the fields of heterocyclic-compound chemistry, materials chemistry, medicinal chemistry, and fluorine chemistry. All information is presented and classified clearly to be effective source for broad auditory of chemists. It will be interesting for scientists working in the field of inorganic and coordination chemistry. Fluorinated heterocycles are becoming increasingly important in many areas including the pharmaceutical industry, materials science and agriculture. The presence of fluorine can result in substantial functional changes in the biological as well as physicochemical properties of organic compounds. Incorporation of fluorine into drug molecules can greatly affect their physicochemical properties, such as bond strength, lipophilicity, bioavailability, conformation, electrostatic potential, dipole moment, pKa etc. as well as pharmacokinetic properties, such as tissue distribution, rate of metabolism and pharmacological properties, such as pharmacodynamics and toxicology.
This text examines the role of fluorine in medicinal chemistry, including anticancer and antiviral agents, and provides up-to-date information on volatile aesthetics and central nervous system agents, areas in which fluorine has played a pivotal role.
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
