Pyrazoles as Key Scaffolds for the Development of Fluorine-18-Labeled Radiotracers for Positron Emission Tomography (PET)

Molecules. 2020 Apr 9;25(7):1722. doi: 10.3390/molecules25071722.

Abstract

The need for increasingly personalized medicine solutions (precision medicine) and quality medical treatments, has led to a growing demand and research for image-guided therapeutic solutions. Positron emission tomography (PET) is a powerful imaging technique that can be established using complementary imaging systems and selective imaging agents-chemical probes or radiotracers-which are drugs labeled with a radionuclide, also called radiopharmaceuticals. PET has two complementary purposes: selective imaging for diagnosis and monitoring of disease progression and response to treatment. The development of selective imaging agents is a growing research area, with a high number of diverse drugs, labeled with different radionuclides, being reported nowadays. This review article is focused on the use of pyrazoles as suitable scaffolds for the development of 18F-labeled radiotracers for PET imaging. A brief introduction to PET and pyrazoles, as key scaffolds in medicinal chemistry, is presented, followed by a description of the most important [18F]pyrazole-derived radiotracers (PET tracers) that have been developed in the last 20 years for selective PET imaging, grouped according to their specific targets.

Keywords: PET probes; fluorine-18; imaging pharmaceuticals; positron emission tomography (PET); pyrazoles; radionuclides.

Publication types

  • Review

MeSH terms

  • Animals
  • Drug Development
  • Fluorine Radioisotopes / chemistry*
  • Humans
  • Ligands
  • Positron-Emission Tomography* / methods
  • Protein Binding
  • Pyrazoles / chemistry*
  • Radioactive Tracers*
  • Radiopharmaceuticals / chemistry*
  • Structure-Activity Relationship

Substances

  • Fluorine Radioisotopes
  • Ligands
  • Pyrazoles
  • Radioactive Tracers
  • Radiopharmaceuticals
  • Fluorine-18