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

Authors
Jeon, Sun AhChoo, HyunahPark, Woo-KyuRhim, HyewhonKo, Soo Y.Cho, Yong SeoKoh, Hun YeongPae, Ae Nim
Issue Date
2007-02-20
Publisher
KOREAN CHEMICAL SOC
Citation
BULLETIN OF THE KOREAN CHEMICAL SOCIETY, v.28, no.2, pp.285 - 291
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 mu M. The compound 2h is novel as 5-HT6 receptor ligand and could act as lead for the novel 5-HT6 receptor ligands.
Keywords
SEROTONIN RECEPTORS; ADENYLATE-CYCLASE; STIMULATION; BINDING; SEROTONIN RECEPTORS; ADENYLATE-CYCLASE; STIMULATION; BINDING; serotonin; 5-HT6 receptor; antagonists
ISSN
0253-2964
URI
https://pubs.kist.re.kr/handle/201004/134641
Appears in Collections:
KIST Article > 2007
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