Synthesis and Biological Evaluation of Arylsulfonylpiperazine Derivatives as 5-HT₆ Receptor Ligands

摘要

The 5-HT₆ antagonists are mainly related to the treatment of cognitive dysfunction or impairment associated with Alzheimer’s disease and schizophrenia. There have been lots of efforts to develop 5-HT₆ antagonists. As in our efforts, arylsulfonylpiperazine derivatives 1-3 were designed, synthesized and biologically evaluated against the human recombinant 5-HT₆ serotonin receptor. Total 36 compounds were synthesized and the most active compound among the synthesized compounds is compound 2h with an IC₅₀ value of 1.5 レM. The compound 2h is novel as 5-HT₆ receptor ligand and could act as lead for the novel 5-HT₆ receptor ligands.