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

doi:10.5012/bkcs.2007.28.2.285

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

Chemistry & Nanoscience

Research output: Contribution to journal › Article › peer-review

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 language	English
Pages (from-to)	285-291
Number of pages	7
Journal	Bulletin of the Korean Chemical Society
Volume	28
Issue number	2
DOIs	https://doi.org/10.5012/bkcs.2007.28.2.285
State	Published - Feb 2007

Keywords

5-HT receptor
Antagonists
Serotonin

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10.5012/bkcs.2007.28.2.285

Cite this

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title = "Synthesis and biological evaluation of arylsulfonylpiperazine derivatives as 5-HT6 receptor ligands",

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.",

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AU - Ko, Soo Y.

AU - Yong, Seo Cho

AU - Hun, Yeong Koh

AU - Ae, Nim Pae

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