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Zirconium ternary complexes with fluoride anions
Zach, Kamil - Lukáš ; Kubíček, Vojtěch (advisor) ; Schulz, Jiří (referee)
Modern medicine uses non-invasive imaging methods for diagnostic purposes. Positron emission tomography is one of them. During the examination, the patient is injected with a radiopharmaceutical that is accumulated in tissue abnormalities and emits detectable radiation during its nuclear decay. The world's most commonly used radionuclide for these purposes is the radioisotope 18 F. The biodistribution of the fluoride ion itself is not very specific, so the radioisotope is usually bound to the structure of bioactive molecules. The actual preparation of these molecules is very challenging, so new labeling methods are currently being sought. One of the new possibilities is the preparation of labeled ternary complexes. In this work, the preparation of two polyazamacrocyclic ligands, H3NOTA and H3PCTA, which have acetate arms attached to their skeleton via aliphatic nitrogen atoms, is described. Zirconium complexes were prepared with these ligands. Subsequently, coordination and dissociation studies of fluoride ions to the prepared complexes were carried out. The measurements were monitored with a fluoride ion selective electrode. Both kinetic and thermodynamic aspects of coordination and decoordination were investigated in the measurements. Furthermore, characterization of the prepared ternary...
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Bifunctional chelators for selective copper(II) binding
Paúrová, Monika ; Kotek, Jan (advisor) ; Vojtíšek, Pavel (referee)
Title: Bifunctional chelators for selective copper(II) binding Autor: Bc. Monika Paúrová Department: Department of Inorganic Chemistry, Faculty of Science Supervisor: doc. RNDr. Jan Kotek, Ph.D. Supervisor's e-mail: modrej@natur.cuni.cz Abstract: In this Master thesis, cyclam bifunctional derivatives bearing pendant phosphinate groups (4-methyl-11-p-aminobenzyl-1,4,8,11-tetraazacyclotetradecane-1,8- bis(methylenephosphinic acid)) and phosphonate groups (4-methyl-11-p-aminobenzyl- 1,4,8,11-tetraazacyclotetradecane-1,8-bis(methylenephosphonic acid)), were prepared and studied as potential ligands for complexation of divalent copper. These ligands are suitable for binding to a macromolecular carrier. Keywords: radiomedicine, copper, cyclam, chelating agent, phosphinate, phosphonate, kinetic inertness, kinetic lability, thermodynamic stability
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New ligands for applications in medicine
Holá, Kateřina ; Kotek, Jan (advisor) ; Holzhauser, Petr (referee)
The aim of this Thesis was the preparation of macrocyclic ligands (Figure 1) for the complexation of lantanoides 3+ . Their complexes can be used in nuclear medicine (in case of ligand L1) or as MRI contrast agents (in case of ligand L2). Ligand L1 was designed to increase the rate of complexation due to the weakly binding pendant group based on iminodiacetic acid (IDA). The complexation mechanism was spectrophotometrically studied with Ce3+ . Spectrophotometric kinetic measurements proved that ligand L1 not only shown no improvement in the complexation rate but its complexation is rather noticeable slowed. Ligand L2 contains amino group whose protonization/coordination could be influenced by pH or temperature. It can be utilized in determination of physical status of different tissues. However, it is difficult to obtain the ligand L2 in sufficient purity for further studies N N NN COOHHOOC HOOC N COOH COOH P OH O L1 N N NN COOHHOOC HOOC NH2 L2 Figure 1: Ligands prepared in course of this Bc Thesis
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Bifunctional ligands for copper(II) complexation
Blahut, Jan ; Kotek, Jan (advisor) ; Svoboda, Jan (referee)
Because of an indisputable pharmacological advatages of radiometal-labeled compounds, a purpose of this work it to design and synthesize a new chelatation system for copper(II) complexation. The solution properties of the ligand and copper complex are also studied, as well as its ability for binding a targeting molecule.
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Bifunctional ligands for copper(II) complexation
Benešová, Martina ; Kotek, Jan (advisor) ; Kozempel, Ján (referee)
Title: Bifunctional ligands for copper(II) complexation Author: Bc. Martina Benešová Supervisor: doc. RNDr. Jan Kotek, Ph.D. Institution: Department of Inorganic Chemistry, Faculty of Science, CU in Prague Author's e-mail: EvaGlaser@seznam.cz ABSTRACT The main aim of this thesis was preparation of macrocyclic ligands based on 1,4,8,11- tetraazacyclotetradecane skeleton, which is suitable for selective complexation of divalent copper, and study of their properties. These ligands are suggested for potential utilization in nuclear medicine. Cyclam macrocycle was modified to bear one coordinating aminobenzylphospinate pendant arm (compound L1) or monophosphinate-bis(phosphonate) pendant arm (compound L2). During the synthesis, the skeleton was protected in positions 1, 4 and 8. In the frame of this work the synthesis of both targeted products was developed. Furthermore, a study of the thermodynamic, kinetic and coordination properties of ligand L2 was investigated by UV/VIS spectrophotometry and potentiometric titrations. A model bioconjugation of ligand L1 with primary amine was also studied. KEYWORDS Cyclam, phosphinates, phosphonates, nuclear medicine, copper(II) complexes, kinetic inertness, thermodynamic stability.
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Bifunctional ligands for copper(II) complexation
Benešová, Martina ; Kotek, Jan (advisor) ; Kozempel, Ján (referee)
Title: Bifunctional ligands for copper(II) complexation Author: Bc. Martina Benešová Supervisor: doc. RNDr. Jan Kotek, Ph.D. Institution: Department of Inorganic Chemistry, Faculty of Science, CU in Prague Author's e-mail: EvaGlaser@seznam.cz ABSTRACT The main aim of this thesis was preparation of macrocyclic ligands based on 1,4,8,11- tetraazacyclotetradecane skeleton, which is suitable for selective complexation of divalent copper, and study of their properties. These ligands are suggested for potential utilization in nuclear medicine. Cyclam macrocycle was modified to bear one coordinating aminobenzylphospinate pendant arm (compound L1) or monophosphinate-bis(phosphonate) pendant arm (compound L2). During the synthesis, the skeleton was protected in positions 1, 4 and 8. In the frame of this work the synthesis of both targeted products was developed. Furthermore, a study of the thermodynamic, kinetic and coordination properties of ligand L2 was investigated by UV/VIS spectrophotometry and potentiometric titrations. A model bioconjugation of ligand L1 with primary amine was also studied. KEYWORDS Cyclam, phosphinates, phosphonates, nuclear medicine, copper(II) complexes, kinetic inertness, thermodynamic stability.
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Bifunctional chelators for selective copper(II) binding
Paúrová, Monika ; Kotek, Jan (advisor) ; Vojtíšek, Pavel (referee)
Title: Bifunctional chelators for selective copper(II) binding Autor: Bc. Monika Paúrová Department: Department of Inorganic Chemistry, Faculty of Science Supervisor: doc. RNDr. Jan Kotek, Ph.D. Supervisor's e-mail: modrej@natur.cuni.cz Abstract: In this Master thesis, cyclam bifunctional derivatives bearing pendant phosphinate groups (4-methyl-11-p-aminobenzyl-1,4,8,11-tetraazacyclotetradecane-1,8- bis(methylenephosphinic acid)) and phosphonate groups (4-methyl-11-p-aminobenzyl- 1,4,8,11-tetraazacyclotetradecane-1,8-bis(methylenephosphonic acid)), were prepared and studied as potential ligands for complexation of divalent copper. These ligands are suitable for binding to a macromolecular carrier. Keywords: radiomedicine, copper, cyclam, chelating agent, phosphinate, phosphonate, kinetic inertness, kinetic lability, thermodynamic stability
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Bifunctional ligands for copper(II) complexation
Blahut, Jan ; Kotek, Jan (advisor) ; Svoboda, Jan (referee)
Because of an indisputable pharmacological advatages of radiometal-labeled compounds, a purpose of this work it to design and synthesize a new chelatation system for copper(II) complexation. The solution properties of the ligand and copper complex are also studied, as well as its ability for binding a targeting molecule.
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New ligands for applications in medicine
Holá, Kateřina ; Holzhauser, Petr (referee) ; Kotek, Jan (advisor)
The aim of this Thesis was the preparation of macrocyclic ligands (Figure 1) for the complexation of lantanoides 3+ . Their complexes can be used in nuclear medicine (in case of ligand L1) or as MRI contrast agents (in case of ligand L2). Ligand L1 was designed to increase the rate of complexation due to the weakly binding pendant group based on iminodiacetic acid (IDA). The complexation mechanism was spectrophotometrically studied with Ce3+ . Spectrophotometric kinetic measurements proved that ligand L1 not only shown no improvement in the complexation rate but its complexation is rather noticeable slowed. Ligand L2 contains amino group whose protonization/coordination could be influenced by pH or temperature. It can be utilized in determination of physical status of different tissues. However, it is difficult to obtain the ligand L2 in sufficient purity for further studies N N NN COOHHOOC HOOC N COOH COOH P OH O L1 N N NN COOHHOOC HOOC NH2 L2 Figure 1: Ligands prepared in course of this Bc Thesis
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