|
|
Coordination behaviour of substituted cyclen derivatives
Bárta, Jiří ; Kotek, Jan (advisor) ; Vargová, Zuzana (referee) ; Lubal, Přemysl (referee)
Magnetic resonance imaging (MRI) is one of the none-invasive techniques of human body examination. The only disadvantage of MRI is a low resolution and specificity, therefore, MRI contrast agents (CAs) are widely used in clinical practice (approximately in 40 % of all examinations). They increase not only resolution and specificity but also efficiency of the examination. The CAs consist of paramagnetic ion (Gd3+ or Mn2+ ) and strong chelator such as H4DOTA. Macrocycle cyclen (1,4,7,10-tetraazacyclododecane) is basis of many derivatives which are being used, including mentioned the H4DOTA ligand. 1,4-phosphonic or 1,4-phosphinic acid cyclen derivatives could be a better alternative to commercially available ones. In this thesis, a synthetic pathway to 5 of these novel derivatives is introduced. The protonation constants and stability constants with metals used in CAs (Mn2+ , Gd3+ ) and other selected ones using the potentiometric titrations are determined for 1,4-H4DO2P, 1,4-H2DO2POEt and 1,4-H2DO2Bn2PH . All three ligands have higher stability constant with Mn2+ - log KLM around 12, than with Ca2+ - log KLM around 8, which is the closest rival for transmetallation under physiological conditions. Strong Gd3+ -complex is formed by hexadentate ligand 1,4-H4DO2P - log KLM = 19.15, which is comparable...
|
|
|
Coordination behaviour of substituted cyclen derivatives
Bárta, Jiří ; Kotek, Jan (advisor) ; Vargová, Zuzana (referee) ; Lubal, Přemysl (referee)
Magnetic resonance imaging (MRI) is one of the none-invasive techniques of human body examination. The only disadvantage of MRI is a low resolution and specificity, therefore, MRI contrast agents (CAs) are widely used in clinical practice (approximately in 40 % of all examinations). They increase not only resolution and specificity but also efficiency of the examination. The CAs consist of paramagnetic ion (Gd3+ or Mn2+ ) and strong chelator such as H4DOTA. Macrocycle cyclen (1,4,7,10-tetraazacyclododecane) is basis of many derivatives which are being used, including mentioned the H4DOTA ligand. 1,4-phosphonic or 1,4-phosphinic acid cyclen derivatives could be a better alternative to commercially available ones. In this thesis, a synthetic pathway to 5 of these novel derivatives is introduced. The protonation constants and stability constants with metals used in CAs (Mn2+ , Gd3+ ) and other selected ones using the potentiometric titrations are determined for 1,4-H4DO2P, 1,4-H2DO2POEt and 1,4-H2DO2Bn2PH . All three ligands have higher stability constant with Mn2+ - log KLM around 12, than with Ca2+ - log KLM around 8, which is the closest rival for transmetallation under physiological conditions. Strong Gd3+ -complex is formed by hexadentate ligand 1,4-H4DO2P - log KLM = 19.15, which is comparable...
|
guest ::
