N₁-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole derivatives are potent and selective 5-HT₆ receptor antagonists

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• 作者：Cole ; Derek C. ; Ellingboe ; John W. ; Lennox ; William J. ; Mazandarani ; Hossein ; Smith ; Deborah L. ; et. al.
• 关键词：5-HT₆ antagonists ; 5-Hydroxytryptamine₆ antagonists
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2005
• 出版时间：January 17, 2005
• 年：2005
• 卷：15
• 期：2
• 页码：379-383
• 全文大小：284 K

文摘

A series of N₁-arylsulfonyl-3-(1,2,3,6-tetrahydropyridin-4-yl)indole derivatives was designed and synthesized. These compounds were shown to have high affinity for the 5-HT₆ receptor. Two analogs, 4-[3-(1,2,3,6-tetrahydropyridin-4-yl)-1H-indole-1-sulfonyl]-phenylamine 15g and 4-[3-(1,2,3,6-tetrahydropyridin-4-yl)-5-methoxy-1H-indole-1-sulfonyl]-phenylamine 15y, had 0.4 and 3.0nM affinity, respectively, and antagonized the production of adenylate cyclase at sub-nanomolar concentrations.