Synthesis and biological evaluation of benzoisothiazole derivatives possessing N,N-dimethylformimidamide group as 5-HT₆ receptor antagonists

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• 作者：Euna Yoo^a ; Faisal Hayat^a ; Hyewhon Rhim^b ; ^{hrhim@kist.re.kr} ; Hea-Young Park Choo^a ; ^{hypark@ewha.ac.kr}
• 关键词：5-HT6 receptor antagonists ; Benzoisothiazole ; Sulfonamide ; N ; N-dimethylformimidamide
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2012
• 期刊代码：9_09680896
• 类别：ch
• 出版时间：15 April, 2012
• 卷：20
• 期：8
• 页码：2707-2712
• 文件大小：287 K

摘要

A series of novel N,N-dimethyl-N鈥?(5-(Ar-sulfonamido) benzo[d]isothiazol-3-yl)formimidamides was designed and synthesized as 5-HT₆ ligands. Here N,N-dimethyl formimidamides was used as a replacement for an aminoethyl moiety. In vitro functional assays demonstrated compounds 9b and 9i significantly inhibited the 5-HT-induced Ca²⁺ increases (9b; IC₅₀ = 0.36 渭M and 9i; IC₅₀ = 0.44 渭M), indicating that 9b and 9i were potent 5-HT₆ receptor antagonists. Compounds 9i also showed good selectivity on the 5-HT₆ over 5-HT₄ and 5-HT₇ receptors.