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Bulletin of the Korean Chemical Society (BKCS)

ISSN 0253-2964(Print)
ISSN 1229-5949(Online)
Volume 28, Number 2
BKCSDE 28(2)
February 20, 2007

Title	Synthesis and Biological Evaluation of Arylsulfonylpiperazine Derivatives as 5-HT₆ Receptor Ligands
Author	Sun Ah Jeon, Hyunah Choo, Woo-Kyu Park, Hyewhon Rhim, Soo Y. Ko, Yong Seo Cho, Hun Yeong Koh, Ae Nim Pae*
Keywords	Serotonin, 5-HT₆ Receptor, Antagonists
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.
Page	285 - 291
Full Text	PDF

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