In order to improve the cognitive-behavioral pathway, and based on a well-established history of city-hospital collaboration, a monthly staff meeting bringing together hospital and out-of-hospital professionals and a users' association makes it possible to analyze and respond in a coordinated and graduated manner to complex situations. After nine months of operation, the story of three complex situations illustrates the benefits and limits of such a system.
View Article and Find Full Text PDFA robust, click-chemistry-inspired procedure for radiolabeling of cyclic ureas was developed. This protocol, suitable for all carbon isotopes ( C, C, C), is based on the direct functionalization of carbon dioxide: the universal building block for carbon radiolabeling. The strategy is operationally simple and reproducible in different radiochemistry centers, exhibits remarkably wide substrate scope with short reaction times, and demonstrates superior reactivity as compared to previously reported systems.
View Article and Find Full Text PDFThe acid-base and copper(ii) coordination properties of three previously described cyclam derivatives are reported. Potentiometry, mass spectrometry, UV-vis absorption spectroscopy, electrochemistry and theoretical calculations were combined to investigate the protonation and binding properties of Bn-cyclam-EtOH (L1), oxo-cyclam-EtOH (L2) and oxo-Bn-cyclam-EtOH (L3). These three cyclams are C-functionalized by a hydroxyethyl pendant arm and display either one N-benzyl group and/or an amide replacing one macrocyclic secondary amine.
View Article and Find Full Text PDFCorrection for 'New synthesis of phenyl-isothiocyanate C-functionalised cyclams. Bioconjugation and 64Cu phenotypic PET imaging studies of multiple myeloma with the te2a derivative' by Zakaria Halime et al., Org.
View Article and Find Full Text PDFAzamacrocyclic bifunctional chelating agents (BCAs) are essential for the development of radiopharmaceuticals in nuclear medicine and we wish to prove that their bioconjugation by a function present on a carbon atom of the macrocyclic skeleton is a solution of choice to maintain their in vivo inertness. Based on our very recent methodology using a bisaminal template and selective N-alkylation approach, a new synthesis of conjugable C-functionalised teta, te2a and cb-te2a has been developed. These chelators have indeed a growing interest in nuclear medicine for positron emission tomography (PET) and radioimmunotherapy (RIT) where they show in several cases better complexation properties than dota or dota-like macrocycles, especially with (64)Cu or (67)Cu radioisotopes.
View Article and Find Full Text PDFThe investigation of iron oxide-based positron emission tomography/magnetic resonance (PET/MR) multimodal imaging agents is an expanding field in which a variety of nanoparticle sizes, shapes, surface coatings and radioisotopes are open for exploration. This study develops iron oxide nanorods which are coated with various mixtures of poly(ethylene glycol) (PEG) and macrocyclic ligand (DO3A) via the formation of a silica layer on the surface. Gallium-68 radiolabelling of the nanorods was carried out in high radiochemical yields (RCY) and their stability in human serum was demonstrated for all constructs, even in the absence of the macrocyclic chelating unit.
View Article and Find Full Text PDFWe report the synthesis of the ligand Hnompa (6-((1,4,7-triazacyclononan-1-yl)methyl)picolinic acid) and a detailed characterization of the Mn(2+) complexes formed by this ligand and the related ligands Hdompa (6-((1,4,7,10-tetraazacyclododecan-1-yl)methyl)picolinic acid) and Htempa (6-((1,4,8,11-tetraazacyclotetradecan-1-yl)methyl)picolinic acid). These ligands form thermodynamically stable complexes in aqueous solution with stability constants of logKMnL = 10.28(1) (nompa), 14.
View Article and Find Full Text PDFThe synthesis of a new cross-bridged 1,4,8,11-tetraazacyclotetradecane (cb-cyclam) derivative bearing a picolinate arm (Hcb-te1pa) was achieved by taking advantage of the proton sponge properties of the starting constrained macrocycle. The structure of the reinforced ligand as well as its acid-base properties and coordination properties with Cu(2+) and Zn(2+) was investigated. The X-ray structure of the free ligand showed a completely preorganized conformation that lead to very fast copper(II) complexation under mild conditions (instantaneous at pH 7.
View Article and Find Full Text PDFWe describe an easy synthesis of original C-functionalized cyclam derivatives based on the efficient bisaminal template method. In the perspective of developing bifunctional chelating agents (BCAs), this new synthetic strategy offers the possibility of introducing various coupling functions on one carbon atom in the β-N position of the macrocycle, leaving the four nitrogen atoms available for the introduction of pendant coordinating arms. The methodology is based on a keystone C-functionalized oxo-cyclam bisaminal intermediate that is obtained by cyclization of a preorganized tetraamine using various methyl acrylate analogues.
View Article and Find Full Text PDFIntroduction: HTE1PA, a monopicolinate-N-alkylated cyclam-based ligand has previously demonstrated fast complexation process, high kinetic inertness and important thermodynamic and electrochemical stability with respect to natural copper. In this work we first developed a new synthetic route to obtain HTE1PA in good yields. Then, we investigated HTE1PA chelation properties towards copper-64 and assessed in vitro and in vivo stability of the resulting compound.
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