Design and synthesis of 1-(2-alkanamidoethyl)-6-methoxy-7-azaindole derivatives as potent melatonin agonists
| Autor: | Franck Suzenet, Philippe Delagrange, Matthieu Jeanty, Olivier Nosjean, Jean A. Boutin, Daniel Henri Caignard, Gérald Guillaumet |
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| Rok vydání: | 2011 |
| Předmět: |
Agonist
Indoles Bicyclic molecule Receptor Melatonin MT2 Chemistry Stereochemistry medicine.drug_class Receptor Melatonin MT1 Organic Chemistry Clinical Biochemistry Pharmaceutical Science Carboxamide Biochemistry Chemical synthesis Affinities Melatonin Drug Design Drug Discovery medicine Molecular Medicine Pharmacophore Receptor Molecular Biology Protein Binding medicine.drug |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 21:2316-2319 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/j.bmcl.2011.02.097 |
| Popis: | 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 MT 1 and MT 2 receptors were evaluated. Compounds 7a – c and 12 (cyclohexyl ring connected at C-2 and C-3 position) appears as important melatonin MT 2 and MT 1 receptors agonists. On the other hand, the presence of basic groups (amines) at position C-3 was detrimental to the melatoninergic affinities. |
| Databáze: | OpenAIRE |
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