Synthesis and Preliminary Screening of Novel Tryptamines as 5-HT4 Receptor Ligands Academic Article uri icon

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.

authors

  • Hanna-Elias, A
  • Manallack, DT
  • Berque-Bestel, I
  • Irving, HR
  • Coupar, IM
  • Iskander, MN

publication date

  • September 1, 2010