New azepino[4,3-b]indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced neurotoxicity

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• 作者：Modesto de Candia ; Giorgia Zaetta ; Nunzio Denora ; Domenico Tricarico ; Maria Majellaro ; Saverio Cellamare ; Cosimo D. Altomare ; ^{cosimodamiano.altomare@uniba.it}
• 关键词：Alzheimer's disease ; Azepino[4 ; 3-b]indole ; Butyrylcholinesterase ; N-Methyl d-aspartate receptor ; Neuroprotection
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：5 January 2017
• 年：2017
• 卷：125
• 期：Complete
• 页码：288-298
• 全文大小：1384 K
• 卷排序：125

文摘

New azepino[4,3-b]indol-1(2H)-one derivatives were synthesized as anti-Alzheimer agents. Compound 12b proved to be very potent as inhibitor of human BChE (IC50 = 13 nM). At micromolar concentrations, 12b showed protective effects against NMDA in SH-SY5Y cells. At the active doses, 12b did not exhibit cytotoxicity on liver HepG2 cells.