Tricyclic azepine derivatives as selective brain penetrant 5-HT₆ receptor antagonists

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• 作者：Giancarlo Trani ; Stuart M. Baddeley ; Michael A. Briggs ; Tsu T. Chuang ; Nigel J. Deeks ; Christopher N. Johnson ; Abir A. Khazragi ; Tania L. Mead ; Andrew D. Medhurst ; Peter H. Milner ; Leann P. Quinn ; Ali
• 关键词：5-HT₆ receptor antagonists ; Conformational constraint ; CNS penetration
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2008
• 出版时间：15 October 2008
• 年：2008
• 卷：18
• 期：20
• 页码：5698-5700
• 全文大小：160 K

文摘

Starting from a benzazepine sulfonamide 5-HT₆ receptor antagonist lead with limited brain penetration, application of a strategy of conformational constraint and reduction of hydrogen bond donor count led to a novel series of tricyclic derivatives with high 5-HT₆ receptor affinity and excellent brain:blood ratios.