Synthesis and Physicochemical Properties of Cefepime Derivatives Suitable for Labeling with Gallium-68

Bone and soft tissue infections are potentially life-threatening and require immediate and intensive treatment. However, there is still no single diagnostic method that can reliably confirm or rule out such conditions. Imaging with radiopharmaceuticals (i.e., scintigraphy) is a powerful diagnostic t...

Full description

Saved in:
Bibliographic Details
Published in:Applied sciences 2023-04, Vol.13 (8), p.5019
Main Authors: Koźmiński, Przemysław, Żelechowska-Matysiak, Kinga, Gniazdowska, Ewa
Format: Article
Language:English
Subjects:
Acids
Antibiotics
Bacterial diseases
Bacterial infections
Blood & organ donations
Cefepime
chelator
Chromatography
Diabetes
Foot diseases
Gallium
Gallium isotopes
gallium-68
Health aspects
Inflammatory diseases
Ligands
Medical imaging
Particle size
Physicochemical properties
Pore size
Radioisotopes
radiolabeling
Scintigraphy
Soft tissues
Solvents
Streptococcus infections
synthesis
Citations: Items that this one cites
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary:Bone and soft tissue infections are potentially life-threatening and require immediate and intensive treatment. However, there is still no single diagnostic method that can reliably confirm or rule out such conditions. Imaging with radiopharmaceuticals (i.e., scintigraphy) is a powerful diagnostic tool in the management of patients with infectious or inflammatory diseases. In this work, a new and efficient way to modify the thiazole ring of the cefepime molecule has been proposed and experimentally verified. The developed organic synthesis routes allow for the coupling of the appropriate complexing ligand of the gallium-68 radionuclide with cefepime. The new NODAGA-Glu-CFM conjugate was radiolabeled with gallium-68 with a high yield and showed full stability in human serum. In addition, the [68Ga]Ga-NODAGA-Glu-CFM radioconjugate was hydrophilic and positively charged. Therefore, on the basis of these results, the [68Ga]Ga-NODAGA-Glu-CFM radioconjugate might be considered as a new promising radioconjugate for the diagnosis of bacterial infections.
ISSN:2076-3417
2076-3417
DOI:10.3390/app13085019