Synthesis and evaluation of fluorine-18 labelled compounds for imaging of bacterial infections with pet. 2006

S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
Institut für Molekulare Biophysik, Radiopharmazie und Nuklearmedizin, Herz- und Diabeteszentrum Nordrhein-Westfalen, Universitaetsklinik der Ruhr-Universitaet, Bochum, Georgstrasse 11, 32545 Bad Oeynhausen, Germany. szijlstra@hdz-nrw.de

Syntheses of no carrier added (n.c.a.) 6-fluoro-1,4-dihydro-1-cyclopropyl-4-oxo-7-[4-[18F]fluoro-phenacyl-1-piperacinyl]-chinolincarboxylic acid ([18F]COPCA) and n.c.a. 4-[18F]fluoro-benzoyl-ubiquicidin 29-41 ([18F]UBI 29-41) are described. [18F]COPCA was synthesised within 120 min with a radiochemical yield of 9-12%. [18F]UBI 29-41 was synthesised within 150 min with a radiochemical yield of 15-20%. Both compounds had a specific activity of more than 35 GBq/micromol. The biological activity was verified by measuring its binding to Staphylococcus aureus bacteria. Specific binding was found for [18F]UBI 29-41 (12-17%), whereas no specific binding for [18F]COPCA was found.

UI MeSH Term Description Entries
D009682 Magnetic Resonance Spectroscopy Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING). In Vivo NMR Spectroscopy,MR Spectroscopy,Magnetic Resonance,NMR Spectroscopy,NMR Spectroscopy, In Vivo,Nuclear Magnetic Resonance,Spectroscopy, Magnetic Resonance,Spectroscopy, NMR,Spectroscopy, Nuclear Magnetic Resonance,Magnetic Resonance Spectroscopies,Magnetic Resonance, Nuclear,NMR Spectroscopies,Resonance Spectroscopy, Magnetic,Resonance, Magnetic,Resonance, Nuclear Magnetic,Spectroscopies, NMR,Spectroscopy, MR
D010879 Piperazines Compounds that are derived from PIPERAZINE.
D011877 Radionuclide Imaging The production of an image obtained by cameras that detect the radioactive emissions of an injected radionuclide as it has distributed differentially throughout tissues in the body. The image obtained from a moving detector is called a scan, while the image obtained from a stationary camera device is called a scintiphotograph. Gamma Camera Imaging,Radioisotope Scanning,Scanning, Radioisotope,Scintigraphy,Scintiphotography,Imaging, Gamma Camera,Imaging, Radionuclide
D002851 Chromatography, High Pressure Liquid Liquid chromatographic techniques which feature high inlet pressures, high sensitivity, and high speed. Chromatography, High Performance Liquid,Chromatography, High Speed Liquid,Chromatography, Liquid, High Pressure,HPLC,High Performance Liquid Chromatography,High-Performance Liquid Chromatography,UPLC,Ultra Performance Liquid Chromatography,Chromatography, High-Performance Liquid,High-Performance Liquid Chromatographies,Liquid Chromatography, High-Performance
D005462 Fluorine Radioisotopes Unstable isotopes of fluorine that decay or disintegrate emitting radiation. F atoms with atomic weights 17, 18, and 20-22 are radioactive fluorine isotopes. Radioisotopes, Fluorine
D000900 Anti-Bacterial Agents Substances that inhibit the growth or reproduction of BACTERIA. Anti-Bacterial Agent,Anti-Bacterial Compound,Anti-Mycobacterial Agent,Antibacterial Agent,Antibiotics,Antimycobacterial Agent,Bacteriocidal Agent,Bacteriocide,Anti-Bacterial Compounds,Anti-Mycobacterial Agents,Antibacterial Agents,Antibiotic,Antimycobacterial Agents,Bacteriocidal Agents,Bacteriocides,Agent, Anti-Bacterial,Agent, Anti-Mycobacterial,Agent, Antibacterial,Agent, Antimycobacterial,Agent, Bacteriocidal,Agents, Anti-Bacterial,Agents, Anti-Mycobacterial,Agents, Antibacterial,Agents, Antimycobacterial,Agents, Bacteriocidal,Anti Bacterial Agent,Anti Bacterial Agents,Anti Bacterial Compound,Anti Bacterial Compounds,Anti Mycobacterial Agent,Anti Mycobacterial Agents,Compound, Anti-Bacterial,Compounds, Anti-Bacterial
D012269 Ribosomal Proteins Proteins found in ribosomes. They are believed to have a catalytic function in reconstituting biologically active ribosomal subunits. Proteins, Ribosomal,Ribosomal Protein,Protein, Ribosomal
D013203 Staphylococcal Infections Infections with bacteria of the genus STAPHYLOCOCCUS. Infections, Staphylococcal,Staphylococcus aureus Infection,Staphylococcal Infection,Staphylococcus aureus Infections
D015363 Quinolones A group of derivatives of naphthyridine carboxylic acid, quinoline carboxylic acid, or NALIDIXIC ACID. Ketoquinoline,Ketoquinolines,Oxoquinoline,Oxoquinolines,Quinolinone,Quinolinones,Quinolone
D019275 Radiopharmaceuticals Compounds that are used in medicine as sources of radiation for radiotherapy and for diagnostic purposes. They have numerous uses in research and industry. (Martindale, The Extra Pharmacopoeia, 30th ed, p1161) Radiopharmaceutical

Related Publications

S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
December 2014, Angewandte Chemie (International ed. in English),
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
March 2024, EJNMMI radiopharmacy and chemistry,
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
July 2017, Chemical Society reviews,
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
June 2022, Molecules (Basel, Switzerland),
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
January 2014, Bioorganic & medicinal chemistry letters,
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
August 2011, Bioorganic & medicinal chemistry,
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
October 2000, European journal of nuclear medicine,
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
February 2012, Bioorganic & medicinal chemistry letters,
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
May 2021, Chemical communications (Cambridge, England),
S Zijlstra, and J Gunawan, and C Freytag, and W Burchert
August 2002, Bioorganic & medicinal chemistry,
Copied contents to your clipboard!