Synthesis and biological evaluation of arylsulfonylpiperazine derivatives as 5-HT6 receptor ligands

Ah Jeon Sun, Hyunah Choo, Woo Kyu Park, Hyewhon Rhim, Soo Y. Ko, Seo Cho Yong, Yeong Koh Hun, Nim Pae Ae

Research output: Contribution to journalArticlepeer-review

1 Scopus citations

Abstract

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 μM. The compound 2h is novel as 5-HT6 receptor ligand and could act as lead for the novel 5-HT6 receptor ligands.

Original languageEnglish
Pages (from-to)285-291
Number of pages7
JournalBulletin of the Korean Chemical Society
Volume28
Issue number2
DOIs
StatePublished - Feb 2007

Keywords

  • 5-HT receptor
  • Antagonists
  • Serotonin

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