Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371144 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
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.
Graphical abstractNew potent melatonin agonists based on a 7-azaindole scaffold are reported, along with some affinities-dependent pharmacomodulations.Figure optionsDownload full-size imageDownload as PowerPoint slide
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Matthieu Jeanty, Franck Suzenet, Philippe Delagrange, Olivier Nosjean, Jean A. Boutin, Daniel H. Caignard, Gérald Guillaumet,