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Conception, synthèse et évaluation biologique de nouveaux ligands sérotoninergiques 5-HT₇

Abstract : Serotonin-activated cell-surface receptor 5-HT₇ is the most recently discovered 5-HT receptor. Intensive studies of structure-activity relationships have been pursued by several research groups, including our laboratory, and have resulted in the publication in the literature of an impressive number of potential ligands 5-HT₇. In this context, the main purpose of this thesis is to design four distinct classes of ligands. First, we were interested in the preparation of 2,4-diaminopyrido[2,3-d]pyrimidinique and 2,4-diaminopyrimidinique ligands. Subsequently, we developed a third family of compounds built on a pyridine scaffold, from one of the most interesting current 5-HT₇ selective agonists, via an effective multistep strategy. The last part of this thesis was devoted to developing an original and rapid method for the synthesis of polysubstituted tetrahydro-1,6-naphthyridines starting from the 3-vinyl-1,2,4-triazines platforms via a domino addition sequence of aza-Michael and intramolecular inverse-electron-demand Diels-Alder cyclization.
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Jabrane Jouha. Conception, synthèse et évaluation biologique de nouveaux ligands sérotoninergiques 5-HT₇. Autre. Université d'Orléans, 2017. Français. ⟨NNT : 2017ORLE2013⟩. ⟨tel-01968080⟩

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