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Contrast agents for 19F magnetic resonance imaging
Martinisková, Marie ; Kotek, Jan (advisor) ; Vojtíšek, Pavel (referee)
The aim of this Master Thesis is to synthesize and study new macrocyclic ligands containing fluorine atoms for use as potencial contrast agents in 19 F magnetic resonance imaging. New ligands were designed as analogues of ligands used in contrast agents already utilized in clinical practice - macrocyclic ligand for complexation of trivalent lanthanide ions based on DOTA skeleton and series of macrocyclic ligands for complexation of divalent nickel ion based on cyclam skeleton. All designed ligands were synthesized a characterized. The complexes [LnIII (dotptfe )]− were tested in vitro and in vivo to study 19 F NMR relaxation times enhancements.
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Coordination properties of NOTA monoamide
Kubinec, Jan ; Kubíček, Vojtěch (advisor) ; Matulková, Irena (referee)
The aim of this thesis was to prepare monoamide of macrocycle NOTA, which was successfully prepared and fully characterized. Acid-base properties were investigated by potentiometric titration and four protonation constants were found, which are lower than pKa ` s of NOTA ligand. Coordination properties with selected ions from the first row of transition metals were investigated. Stability constants of studied complexes are also lower than the same complexes with NOTA ligand. Key words: macrocyclic complexes, positron emission tomography, thermodynamic stability, formation kinetic, radiopharmaceuticals
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TACN derivatives bearing aminophosphinate pendant arms
Beranová, Tereza ; Kubíček, Vojtěch (advisor) ; Němec, Ivan (referee)
The aim of this work was studying of the coordination properties of TACN macrocyclic derivatives with aminophosphinate pendant arms. Two ligands were prepared, one with two pendant arms NODPam and one with three pendant arms NOTPam. Because of degradation of ligand NODPam during its synthesis, only the ligand NOTPam was studied further. Acid-base properties of ligand and termodynamic stability of aluminium and gallium complexes were studied. Formation and disociation studies were performed with the complexes. Coordination of fluoride ions to aluminium complex was studied using ion selective fluoride electrode. Finally coordination of complex AlFx with ligand NOTPam was studied using 19F and 27Al NMR spectroscopy. Selected experiments were made also with ligand NOTA. Key words: macrocyclic complexes, positron emission tomography, phosphinic acids
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MRI contrast agents for angiography
Urbanovský, Peter ; Kotek, Jan (advisor) ; Vojtíšek, Pavel (referee)
Modern diagnostic method magnetic resonance imaging (MRI) usually uses contrast agents T1-type, which are based on Gd3+ complexes. Due to severe toxicity of free Gd3+ , it is desired to have thermodynamically stable and kinetically inert complexes with fast elimination from the body. This work summarizes information about a novel contrast agent based on ligand DO3AP (1,4,7,10-tetraazacyclododecane-1-methyl(alkyl)phosphinic-4,7,10- triacetic acid) with pendant hydrophobic dibenzylamino group which is able to interact hydrophobically with the macromolecule of serum albumin. The stability of supracomplex is dependent on pH value, i.e. on the protonation of the pendant amino group of the complex (pKA = 5.6) and this interaction was confirmed from 1 H-NMRD profile and fluorescent analysis. The compound was tested for its angiographic properties in vivo on rat model. Furthermore, other complexes of the ligand with trivalent lanthanides (Nd3+ , Eu3+ , Tb3+ , Dy3+ , Er3+ ) were characterized by various methods (XRD, luminescence, UV-VIS, 1 H-, 17 O- and 31 P-NMR). The cleavage of the benzyl groups affords ligand whose Ln3+ complexes possess pH dependent PARACEST effect. These complexes were characterized by XRD, luminescence and 1 H- and 31 P-NMR. Moreover, the novel ligands with modified length of pendant...
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New ligands for magnetic resonance imaging - pH-resposive contrast agents
Urbanovský, Peter ; Kotek, Jan (advisor) ; Vojtíšek, Pavel (referee)
Fast spread of MRI technique has brought new demands for MRI contrast agents. They are required to be nontoxic, kinetically inert, thermodynamically stable, biologically inactive complexes Gd(III) with high relaxivity (the ability of magnetic compounds to increase the relaxation rates of the surrounding water proton spins), removable from body in unchanged form. This bachelor thesis resumes basic theory for contrast agents, synthesis of new ligand and its Gd(III) complex coordinating one molecule of water and with ability of the non-covalent interaction of benzylic group with serum albumine resulting in increase in relaxivity. Luminiscence were measured for Eu(III) and Tb(III) complexes and relaxivity of Gd(III) complex in and without the presence of bovine serum albumine in vitro. The novel contrast agent was tested in vivo on rat model. Keywords MRI, gadolinium, macrocyclic ligands, macrocyclic complexes
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Contrast agents for 19F magnetic resonance imaging
Martinisková, Marie ; Kotek, Jan (advisor) ; Škoch, Karel (referee)
The aim of this bachelor thesis is to synthesize and study new kind of macrocyclic ligands for Ln3+ ions containing nuclei 19 F for using as possible contrast agents in 19 F magnetic resonance imaging. Prepared ligands were designed as analogues of already known ligands for Ln3+ ions, which are used in clinical practice. Both designed ligads were successfully prepared. Complexes [LnIII (dotptfe )]− were prepared and their structure in aqueous solution was predicted by NMR studies and luminiscence spectroscopy. T1 relaxation times of nuclei 19 F in complexes [LnIII (dotptfe )]− and ligand DOTPtfe were determined.
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Alluminium complexes for biomedical applications
Beranová, Tereza ; Kubíček, Vojtěch (advisor) ; Havlíček, David (referee)
The aim of this work was to prepare ligands of macrocycle TACN with aminophosphinate pendant arms. Two ligands were prepared and fully characterized. A complex of aluminium ion was synthesized with one of the ligand. The complex was used for studying a fluoride coordination by a fluoride ion selective electrode. Key words: macrocyclic complex, positron emission tomography, phosphinic acid
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