Synthesis and structure-activity relationship of 2-(aminoalkyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives: a novel series of 5-HT(2A/2C) receptor antagonists

Bioorg Med Chem Lett. 2004 Jun 7;14(11):2765-71. doi: 10.1016/j.bmcl.2004.03.069.

Abstract

Following the program started at Johnson & Johnson Pharmaceutical Research & Development searching for 5-HT(2A/2C) antagonists we now report on the synthesis of a series of substituted 2-(aminomethyl)-3,3a,8,12b-tetrahydro-2H-dibenzocyclohepta[1,2-b]furan derivatives. The 5-HT2A, 5-HT2C and H1 receptor affinities of the described compounds are reported. The mCCP antagonistic activity of a set of selected molecules is also reported.

MeSH terms

  • Furans / chemical synthesis
  • Furans / pharmacology*
  • Humans
  • Ligands
  • Protein Binding
  • Radioligand Assay
  • Serotonin 5-HT2 Receptor Antagonists*
  • Serotonin Antagonists / chemical synthesis*
  • Serotonin Antagonists / pharmacology
  • Structure-Activity Relationship

Substances

  • Furans
  • Ligands
  • Serotonin 5-HT2 Receptor Antagonists
  • Serotonin Antagonists