Fluorine in pharmaceutical and medicinal chemistry: from biophysical aspects to clinical applications

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 importanceof fluorine in drug discovery and clinical applications. For examples, the reader will discover how fluorine has found its place as a key element improvingdrug 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. INDICE: Section 1: Synthesis and Properties of Fluorinated Nucleobases in DNA and RNA (Holger Gohlke, Jelena Bozilovic and Joachim W Engels); Molecular Interactions of Fluorinated Amino Acids within the Hydrophobic Core of a Coiled Coil Peptide (Toni Vagt, Mario Salwiczek and Beate Koksch); Probing the Binding Affinity and Proteolytic Stability of Trifluoromethyl Peptide Mimics as Protease Inhibitors (Matteo Zanda, Alessandro Volonterio, Monica Sani and SergioDall'Angelo); Trifluoromethyl-Substituted ?-Amino Acids as Solid-State 19F NMR Labels for Structural Studies of Membrane-Bound Peptides (Vladimir S Kubyshkin, Igor V Komarov, Sergii Afonin, Pavel K Mykhailiuk, Stephan L Grage and Anne S Ulrich); Section 2: Fluorine-Containing Pharmaceuticals (Steve Swallow); Applications of Pentafluorosulfanyl Substitution in Life Sciences Research (John T Welch); Strategic Incorporation of Fluorine into Taxoids Anticancer Agents(Antonella Pepe, Liang Sun and Iwao Ojima); Synthesis and Antiviral, Antitumor Activities of Fluorinated Sugar Nucleosides (Feng Zheng, Xiao-Long Qiu and Feng-Ling Qing); Synthesis of Fluorinated Neurotransmitter Analogues (Margit Winkler and David O'Hagan); Section 3: 18F-Radionuclide Chemistry (Romain Bejot and Véronique Gouverneur); 18F-Labelled Tracers for PET Oncology and NeurologyApplications (Sajinder K Luthra and Edward G Robins); 19F NMR: Clinical and Molecular Imaging Applications (Vikram D Kodibagkar, Rami R Hallac, Dawen Zhao,Jian-Xin Yu and Ralph P Mason).

• ISBN: 978-1-84816-634-9
• Editorial: Imperial College
• Encuadernacion: Cartoné
• Páginas: 572
• Fecha Publicación: 26/06/2012
• Nº Volúmenes: 1
• Idioma: Inglés