Fluorine in Medicinal Chemistry and Chemical Biology

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Format: eBook
Pub. Date: 2009-03-01
Publisher(s): Wiley-Blackwell
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Summary

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.

Table of Contents

Introduction
"Unique Properties of Fluorine and Their Relevance to Medicinal Chemistry and Chemical Biology"
Medicinal Chemistry
"Fluorinated Prostanoids: Development of Tafluprost, a New Anti-glaucoma Agent"
"Fluorinated conformationally restricted glutamate analogs for CNS drug discovery and development"
"Fluorinated Inhibitors of Matrix Metalloproteinases"
"Fluoro-Taxoid Anticancer Agents"
"Antimalarial Fluoroartemisinins: Increased Metabolic and Chemical Stability"
"Synthesis and Biological Activity of Fluorinated Nucleosides"
Synthetic methods for medicinal chemistry and chemical biology
"Synthesis of gem-Difluoromethylenated Nucleosides via gem-Difluoromethylene-Containing Building Blocks"
"Recent Advances in the Syntheses of Fluorinated Amino Acids"
"Fluorinated Moieties for Replacement of Amide and Peptide Bonds"
"Perfluorinated Heteroaromatic Systems as Scaffolds for Drug Discovery"
"gem-Difluorocyclopropanes as key building blocks for novel biologically active molecules"
"Fluorous Mixture Synthesis (FMS) of Drug-Like Molecules and Enantiomers, Stereoisomers, and Analogs of Natural Products"
"Fluorine-18 Radiopharmaceuticals"
Applications of fluorinated amino acids and peptides to chemical biology and pharmacology
"Application of Artificial Model Systems to Study the Interactions of Fluorinated Amino Acids within the Native Environment of Coiled Coil Proteins"
"Fluorinated Amino Acids and Biomolecules in Protein Design and Chemical Biology"
"Effects of Fluorination on the Bioorganic Properties of Methionine"
"Structure analysis of membrane-active peptides using 19F-labeled amino acids and solid state NMR"
"Metabolism of Fluorine-containing Drugs using in vivo Magnetic Resonance Spectroscopy"
Appendix
"FDA-Approved Active Pharmaceutical Ingredients Containing Fluorine"
Table of Contents provided by Publisher. All Rights Reserved.

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