Synthesis and Preliminary Screening of Novel Tryptamines as 5-HT4 Receptor Ligands
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.
Document Type: Research Article
Affiliations: Medicinal Chemistry and Drug Action, Monash Institute of Pharmaceutical Sciences, Monash University, 381 Royal Parade, Parkville, Vic. 3053, Australia.
Publication date: September 1, 2010
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