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Synthesis and preliminary screening of novel tryptamines as 5-HT4 receptor ligands
A Hanna-Elias1, D T Manallack, I Berque-Bestel
1Monash Institute of Pharmaceutical Sciences, Monash University, Parkville, Vic., Australia.
Abstract:
For the development of novel 5-HT(4) 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-HT(4) receptor.
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