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Fluorine in Medicinal Chemistry and Chemical Biology

640 pages
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.

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Preface List of Contributors Abbreviations
Introduction: Basic Aspects of Fluorine in Chemistry and Biology  1 Unique Properties of Fluorine and Their Relevance to Medicinal Chemistry and Chemical Biology  Takashi Yamazaki, Takeo Taguchi, and Iwao Ojima
Medicinal Chemistry  2 Fluorinated Prostanoids: Development of Tafl uprost, a New Anti-glaucoma Agent  Yasushi Matsumura
 3 Fluorinated Conformationally Restricted Glutamate Analogues for CNS Drug Discovery and Development  Atsuro Nakazato
Fluorinated Inhibitors of Matrix Metalloproteinases Roberta Sinisi, Monika Jagodzinska, Gabriele Candiani, Florent Huguenot, Monica Sani, Alessandro Volonterio, Raffaella Maffezzoni, and Matteo Zanda
 5 Fluoro-Taxoid Anticancer Agents  Antonella Pepe, Larisa Kuznetsova, Liang Sun, and Iwao Ojima
 6 Antimalarial Fluoroartemisinins: Increased Metabolic and Chemical Stability  JeanPierre Bégué and Danièle BonnetDelpon
Synthesis and Biological Activity of Fluorinated Nucleosides Tokumi Maruyama, Masahiro Ikejiri, Kunisuke Izawa, and Tomoyuki Onishi
pageix xi xv
vi Contents
Synthetic Methods for Medicinal Chemistry and Chemical Biology 8 Synthesisofgem-Difluoromethylenated Nucleosides via gem-Difluoromethylene-containing Building Blocks  WeiDong Meng and FengLing Qing
Recent Advances in the Syntheses of Fluorinated Amino Acids Kenji Uneyama
10 Fluorinated Moieties for Replacement of Amide and Peptide Bonds  Takeo Taguchi and Hikaru Yanai
11 Perfl uorinated Heteroaromatic Systems as Scaffolds for Drug Discovery  David Armstrong, Matthew W. Cartwright, Emma L. Parks, Graham Pattison, Graham Sandford, Rachel Slater, Ian Wilson John A. Christopher, David D. Miller, Paul W. Smith, and Antonio Vong
12gem-Difluorocyclopropanes as Key Building Blocks for Novel Biologically Active Molecules  Toshiyuki Itoh
13 Fluorous Mixture Synthesis (FMS) of Drug-like Molecules and Enantiomers, Stereoisomers, and Analogues of Natural Products  Wei Zhang
14 Fluorine-18Radiopharmaceuticals  Michael R. Kilbourn and Xia Shao
Applications of Fluorinated Amino Acids and Peptides to Chemical Biology and Pharmacology
15ApplicationofArticialModelSystemstoStudytheInteractions of Fluorinated Amino Acids within the Native Environment of Coiled Coil Proteins  Mario Salwiczek, Toni Vagt, and Beate Koksch
16 Fluorinated Amino Acids and Biomolecules in Protein Design and Chemical Biology  He Meng, Ginevra A. Clark, and Krishna Kumar
17 Effects of Fluorination on the Bioorganic Properties of Methionine  John F. Honek
18 Structure Analysis of Membrane-Active Peptides 19 Using F-labeled Amino Acids and Solid-State NMR  Parvesh Wadhwani and Erik Strandberg
Study of Metabolism of Fluorine-containing Drugs UsingIn VivoMagnetic Resonance Spectroscopy Erika Schneider and Roger Lin
Appendix Approved Active Pharmaceutical Ingredients Containing Fluorine Elizabeth Pollina Cormier, Manisha Das, and Iwao Ojima525 Section 1. Fluorine-containing Drugs for Human Use Approved by FDA in the United States Section 2. Fluorine-containing Drugs for Veterinary Use Approved by FDA in the United States