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:Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Vic. 3053, Australia.
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.
