Preparation of piperazine derivatives as 5-HT₇ receptor antagonists

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• 作者：Juhee Yoon ; Eun A Yoo ; Ji-Yeon Kim ; Ae Nim Pae ; Hyewhon Rhim ; Woo-Kyu Park ; Jae Yang Kong ; Hea-Young Park Choo
• 关键词：5-HT₇ receptor antagonists ; Piperazine ; Sulfonamide ; 5-HT_2c receptor antagonists
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2008
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 May 2008
• 卷：16
• 期：10
• 页码：5405-5412
• 文件大小：170 K

摘要

Twenty-four compounds of 4-methoxy-N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] benzene sulfonamides and N-[3-(4-substituted phenyl-piperazine-1-yl)propyl] naphthyl sulfonamides were prepared and evaluated as 5-HT₇ receptor antagonists. Most of the compounds showed the IC₅₀ values of 12–580 nM. Four methyl branched analogues were also obtained, but the activity for methyl branched analogues was almost same as its straight chain congeners. Among the synthesized compounds, 3c showed a good activity on 5-HT₇ receptors and a good selectivity on 5-HT_1a, 5-HT_2a, 5-HT_2c, and 5-HT₆ receptors.