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Design and synthesis of 1-(2-alkanamidoethyl)-6-methoxy-7-azaindole derivatives as potent melatonin agonists |
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| Authors: | Jeanty Matthieu Suzenet Franck Delagrange Philippe Nosjean Olivier Boutin Jean A Caignard Daniel H Guillaumet Gérald |
| Institution: | a Institut de Chimie Organique et Analytique (ICOA), Université d′Orléans, UMR-CNRS 6005, BP 6759, rue de Chartres, 45067 Orléans Cedex 2, France b Département des Sciences Expérimentales, Institut de Recherches Servier, 11 rue des Moulineaux, 92150 Suresnes, France |
| Abstract: | A series of 7-azaindolic ligands bearing a methoxy group and a N-acetyl chain as melatoninergic pharmacophores were synthesized and their binding affinities towards MT1 and MT2 receptors were evaluated. Compounds 7a-c and 12 (cyclohexyl ring connected at C-2 and C-3 position) appears as important melatonin MT2 and MT1 receptors agonists. On the other hand, the presence of basic groups (amines) at position C-3 was detrimental to the melatoninergic affinities. |
| Keywords: | Melatonin 7-Azaindole MT receptors agonists |
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