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

Appl Radiat Isot. 2006 Jul;64(7):802-7. doi: 10.1016/j.apradiso.2006.02.095. Epub 2006 Apr 17.

Abstract

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.

MeSH terms

  • Anti-Bacterial Agents / chemical synthesis*
  • Chromatography, High Pressure Liquid
  • Fluorine Radioisotopes* / chemistry
  • Magnetic Resonance Spectroscopy
  • Piperazines / chemical synthesis*
  • Quinolones / chemical synthesis*
  • Radionuclide Imaging
  • Radiopharmaceuticals / chemical synthesis*
  • Ribosomal Proteins / chemical synthesis*
  • Spectrometry, Mass, Electrospray Ionization
  • Staphylococcal Infections / diagnostic imaging*

Substances

  • Anti-Bacterial Agents
  • Fluorine Radioisotopes
  • Piperazines
  • Quinolones
  • Radiopharmaceuticals
  • Ribosomal Proteins
  • ribosomal protein S30