| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1396835 | European Journal of Medicinal Chemistry | 2009 | 8 Pages |
Abstract
Twenty-three indole-3-methanamines were designed, synthesized and evaluated as ligands for the 5-HT4 receptor. Compounds I-d, I-j, I-o, I-q and I-u showed good affinity at 100 μM and I-o was found to be only 5-fold less potent than the agonists serotonin (1) and 5-methoxytryptamine (2). Substitution on the 3-methanamine nitrogen clearly influenced activity with docking experiments into a homology model of the 5-HT4 receptor showing a range of interactions with these side chain substituents. This modelling work together with the SAR determined in this study has provided promising ideas for future synthetic work.
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Related Topics
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Organic Chemistry
Authors
Amir Hanna-Elias, David T. Manallack, Isabelle Berque-Bestel, Helen R. Irving, Ian M. Coupar, Magdy N. Iskander,