Synthesis and Preliminary Screening of Novel Tryptamines as 5-HT4 Receptor Ligands

Title: Synthesis and Preliminary Screening of Novel Tryptamines as 5-HT4 Receptor Ligands

Volume: 17 Issue: 25

Author(s): A. Hanna-Elias, D.T. Manallack, I. Berque-Bestel, H.R. Irving, I.M. Coupar and M.N. Iskander

Affiliation:

Keywords: 5-HT4 ligands, serotonin, tryptamine, 5-HT4 receptor, medicinal chemistry

Abstract: For the development of novel 5-HT4 receptor ligands we have designed and synthesized two series of 5- methoxytryptamine derivatives varying the substitution on the primary amine. Their biological activities were evaluated in a receptor binding assay where a subset of compounds showed comparable potency to the agonists serotonin and 5- methoxytryptamine. Structure-activity analyses have highlighted promising avenues for further synthetic work and binding modes were proposed by docking these compounds into a homology model of the 5-HT4 receptor.

Cite this article as:

Hanna-Elias A., Manallack D.T., Berque-Bestel I., Irving H.R., Coupar I.M. and Iskander M.N., Synthesis and Preliminary Screening of Novel Tryptamines as 5-HT4 Receptor Ligands, Current Medicinal Chemistry 2010; 17 (25) . https://dx.doi.org/10.2174/092986710791859351