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Guillou, Amaury
Universite de Bretagne Occidentale, Comue Universite Bretagne Loire, Ecole Doctorale No. 596 - Matiere, Molecules et Materiaux, UMR CNRS 6521 Cemca - Chimie, Electrochimie Moleculaire et Chimie Analytique, Equipe Cosm, Groupe thematique Macrocycles azotes et Coordination (France)2018
Universite de Bretagne Occidentale, Comue Universite Bretagne Loire, Ecole Doctorale No. 596 - Matiere, Molecules et Materiaux, UMR CNRS 6521 Cemca - Chimie, Electrochimie Moleculaire et Chimie Analytique, Equipe Cosm, Groupe thematique Macrocycles azotes et Coordination (France)2018
AbstractAbstract
[en] The 1,4,7-triazacyclononane (tacn) is part of the family of polyazamacrocycles, and has the faculty, when appropriately N-functionalized with coordination pendants, to form thermodynamically stable and kinetically inert coordination complexes with transition metals. Thanks to their properties tacn derivatives can be found in numerous applications such as medical imaging. Our group has developed some ligands N-functionalized with picolinate and picolyl pendants for an application in PET imaging and MRI. The first part of this thesis is focused on the development of a new class of bimodal PET-optical imaging and MRI-optical imaging probes based on tacn-picolinate units described in the laboratory. The second part deals with the synthesis of new Cu(II) chelators based on tacn-methylthiazolyl units for a potential application in PET imaging. The corresponding Cu(II) complexes were studied by different analytical and spectroscopic methods in order to evaluate their thermodynamic stabilities and kinetic inertness. The chelators that fulfilled all the criteria imposed by the biological media were selected for an application PET imaging of prostate cancer. Some bifunctional analogues were elaborated so as to incorporate them in radiopharmaceuticals radiolabeled with copper-64. (author)
[fr]
Le 1,4,7-triazacyclononane (tacn) fait partie de la famille des polyazamacrocycles et a la faculte, lorsqu'il est N-fonctionnalise par des groupements coordinants adequats, de former des complexes de coordination stables thermodynamiquement et inertes cinetiquement avec les metaux de transition. C'est pourquoi les derives du tacn trouvent de nombreuses applications dans de nombreux domaines, par exemple celui de l'imagerie medicale. Notre equipe a developpe des ligands N-fonctionnalises par des groupements picolinate et methylpyridine pour des applications en imagerie TEP et IRM. Le premier travail de cette these porte sur l'elaboration de nouvelles sondes bimodales TEP-imagerie optique et IRM-imagerie optique a motifs issus de tacn-picolinate decrits au laboratoire. Une seconde partie est axee sur la synthese de nouveaux chelates du Cu(II) a base de tacn portant des bras methylthiazole pour une potentielle application en imagerie TEP. Les complexes de Cu(II) correspondant ont ete etudies par differentes methodes analytiques et spectroscopiques afin de juger leurs stabilites thermodynamiques et leurs inerties cinetiques. Les chelatants repondant aux criteres imposes par le milieu biologique ont ete selectionnes pour une application en imagerie TEP dans le cadre du cancer de la prostate. Des analogues bifonctionnels ont ainsi ete elabores afin de les incorporer dans des radiopharmaceutiques radiomarques au cuivre-64. (auteur)Original Title
Synthese et coordination de triazacyclononanes et de derives bifonctionnels: vers des applications en imageries medicales
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29 Nov 2018; 309 p; 205 refs.; Available from the INIS Liaison Officer for France, see the INIS website for current contact and E-mail addresses; These Specialite: Chimie Moleculaire et Macromoleculaire
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Miscellaneous
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Thesis/Dissertation
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AZINES, BETA DECAY RADIOISOTOPES, BETA-MINUS DECAY RADIOISOTOPES, BETA-PLUS DECAY RADIOISOTOPES, CARBOXYLIC ACID SALTS, CHEMICAL ANALYSIS, COMPLEXES, COMPUTERIZED TOMOGRAPHY, COPPER ISOTOPES, DIAGNOSTIC TECHNIQUES, DRUGS, ELECTRON CAPTURE RADIOISOTOPES, EMISSION, EMISSION COMPUTED TOMOGRAPHY, HETEROCYCLIC COMPOUNDS, HOURS LIVING RADIOISOTOPES, INTERMEDIATE MASS NUCLEI, ISOTOPES, KINETICS, LABELLED COMPOUNDS, LUMINESCENCE, MATERIALS, NUCLEI, ODD-ODD NUCLEI, ORGANIC COMPOUNDS, ORGANIC NITROGEN COMPOUNDS, PHOTON EMISSION, PYRIDINES, QUANTITATIVE CHEMICAL ANALYSIS, RADIOACTIVE MATERIALS, RADIOISOTOPES, REACTION KINETICS, TITRATION, TOMOGRAPHY, TRANSITION ELEMENT COMPLEXES, VOLUMETRIC ANALYSIS
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