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Trivalent and tetravalent metal complexes for radiodiagnostics
Hacaperková, Eliška ; Kubíček, Vojtěch (advisor) ; Drahoš, Bohuslav (referee) ; Polášek, Miloslav (referee)
Fluorine-18 is the most utilized nucleus for positron emission tomography (PET). In 2009, incorporation of fluorine-18 to the coordination sphere of Al(III) was introduced as a new alternative for commonly employed compounds with F-C bond. Such a radiotracer consists of two parts: a metal complex with a fluoride and a peptide or a small/part of biomolecule. Shortly after that, first clinical studies showed a promising potential of such com- pounds for clinical use. Despite a great number of papers dealing with this issue, the research is mostly application-driven and focused on the peptide part of the molecule responsible for specific accumulation within the organism. Studies oriented on a sta- bility of metal-ligand-fluorine ternary system are rather rare and only very little is known about such a three-component system from a chemical point of view in gen- eral. However, stability of F-Al bond strongly dependents on the chemical structure of other ligands in the coordination sphere. Pendant arms of a hexadentate ligand (usually used for Al(III) complexation, e.g., H3NOTA) can compete with fluoride and cause its release which leads to unspecific radioactivity accumulation. Lower ligand denticity should increase the F-Al bond stability, but can decrease the stability of the whole complex at the...
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Design and synthesis of selective gallium(III) chelators
Krchová, Tereza ; Kotek, Jan (advisor) ; Lorenc, Miroslav (referee)
This bachelor thesis is focused on the preparation of two new ligands (based on the 1-oxa-4,7-diazacyclononane skeleton), which would be potentially suitable for fast and selective complexation of Ga(III). Complexes of these ligands could find applications in radiodiagnostics (PET, SPECT), or as a new class of contrast agents for MRI based on proton chemical exchange saturation transfer (CEST). This thesis also describes the preparation of 1-oxa-4,7-diazacyclononane and attempts of preparation of N-benzyloxycarbonylaziridine. Thesis also includes a description of radiodiagnostic and radiotherapeutic methods of nuclear medicine. It also discusses the method of magnetic resonance tomography (MRI), especially the method using CEST contrast agents. Thesis contains an overview of the use of Ga(III) radioisotopes in radiomedicine.
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Design and synthesis of selective gallium(III) chelators
Krchová, Tereza ; Lorenc, Miroslav (referee) ; Kotek, Jan (advisor)
This bachelor thesis is focused on the preparation of two new ligands (based on the 1-oxa-4,7-diazacyclononane skeleton), which would be potentially suitable for fast and selective complexation of Ga(III). Complexes of these ligands could find applications in radiodiagnostics (PET, SPECT), or as a new class of contrast agents for MRI based on proton chemical exchange saturation transfer (CEST). This thesis also describes the preparation of 1-oxa-4,7-diazacyclononane and attempts of preparation of N-benzyloxycarbonylaziridine. Thesis also includes a description of radiodiagnostic and radiotherapeutic methods of nuclear medicine. It also discusses the method of magnetic resonance tomography (MRI), especially the method using CEST contrast agents. Thesis contains an overview of the use of Ga(III) radioisotopes in radiomedicine.
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