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Coordination chemistry of pharmaceuticals
Malová, Zuzana ; Lukeš, Ivan (advisor) ; Vojtíšek, Pavel (referee)
Present methods for diagnosis of neurodegenerative diseases are rather limited and in clinical practise are missing. This thesis is focused on utilization of the positron emission tomography using isotope 64 Cu(II). For the project, two contrast agents were proposed containing ligand for Cu (II) coordination and thioflavine T derivative as fluorescent dye, also as a targeting compound. Structure of the thioflavine T derivative was defined by X-ray structural analysis. The selected fluorescent dye has a high affinity for incipient amyloids and, when bound to their structure, has enhanced fluorescent properties. The proposed ligands are tetraazacyclic. The first one is a diamide, where the thioflavin T derivative is part of a macrocyclic ring. The second selected ligand is linked to the thioflavin T derivative via a linker. Key words: complexes; pharmaceuticals; transition metals
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Coordination chemistry of pharmaceuticals
Malová, Zuzana ; Lukeš, Ivan (advisor) ; Vojtíšek, Pavel (referee)
Present methods for diagnosis of neurodegenerative diseases are rather limited and in clinical practise are missing. This thesis is focused on utilization of the positron emission tomography using isotope 64 Cu(II). For the project, two contrast agents were proposed containing ligand for Cu (II) coordination and thioflavine T derivative as fluorescent dye, also as a targeting compound. Structure of the thioflavine T derivative was defined by X-ray structural analysis. The selected fluorescent dye has a high affinity for incipient amyloids and, when bound to their structure, has enhanced fluorescent properties. The proposed ligands are tetraazacyclic. The first one is a diamide, where the thioflavin T derivative is part of a macrocyclic ring. The second selected ligand is linked to the thioflavin T derivative via a linker. Key words: complexes; pharmaceuticals; transition metals
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Prion Diseases - a role of transition metal ions
Malová, Zuzana ; Lukeš, Ivan (advisor) ; Moško, Tibor (referee)
Prion diseases are widely spread diseases among mammalians. They are characterized by a change of prion protein structure PrPC (cellular, native state) to PrPSc (scrapie, structure typical for prion diseases). It is a change at secondary structure of protein from α-helical to β-sheet structure, which aggregates in brain. One possibility, why it happens is higher transitional metal ions concentration (Zn(II), Cu(II), Fe(III)) in the brain, which bind to PrPC and affects its structure. Aim of this thesis is a synthesis one of protentional drugs based on 2-aminothiazole and its modification to bind fluorescent or radiochemical markers and in future study of its possible interaction with transition metal ions. Key words: complexes; macrocyclic ligands; copper; prion diseases
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