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

Abstract : Among all the neurotransmitters identified up-to-date, serotonin (5-Hydroxytryptamine, 5-HT) is mediated by the most complex system of receptors. The 5-HT7 receptors are the latest discovered (1993) and have many implications both in the central nervous system and in peripheral tissues. The therapeutic potential of new 5- HT7 ligands, selective over the other GPCRs, motivated our research project. Our studies were focused on the design of three different classes of 5-HT7 ligands. The first class was built on a benzimidazolone scaffold. Various modulations afforded a shift of the affinity profile from the 5-HT1ARs to the 5-HT7Rs. A second class of 3-aminofuro- or pyrano[2,3-b]pyridines are in fact the heteroanalogues of one of the most interesting current 5-HT7 selective agonists: the 3-aminochromans. Their synthesis involved an intramolecular Diels-Alder cycloaddition key step starting from a 1,2,4-triazine judiciously substituted in 3 with a convenient aminoalkynol. The developed methodology afforded the variation of the substituents on the amine moiety, of the aromatic substituent and its position on the pyridinic core and of the non-aromatic ring size. A last class of bisarylic derivatives further explored the SAR tendencies of this type of 5-HT7 ligands by modulating the main aromatic scaffold in the benzene, pyrimidine and 1,2,4-triazine series.
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Submitted on : Monday, May 3, 2010 - 6:51:06 PM
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  • HAL Id : tel-00480279, version 1



Eduard Badarau. Conception, synthèse et évaluation biologique de nouvelles classes de ligands sérotoninergiques 5-HT7. Autre. Université d'Orléans, 2009. Français. ⟨NNT : 2009ORLE2002⟩. ⟨tel-00480279⟩



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