N-Propargylpiperidines with naphthalene-2-carboxamide or naphthalene-2-sulfonamide moieties: Potential multifunctional anti-Alzheimer’s agents

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• 作者：Urban Ko&scaron ; ak^a ; Damijan Knez^a ; Nicolas Coquelle^b ; Boris Brus^a ; Anja Pi&scaron ; lar^a ; Florian Nachon^c ; Xavier Brazzolotto^c ; Janko Kos^a ; Jacques-Philippe Colletier^b ; Stanislav Gobec^a ; ^{stanislav.gobec@ffa.uni-lj.si}
• 关键词：Multitarget-directed ligands ; Butyrylcholinesterase inhibitors ; MAO-B inhibitors ; Alzheimer&rsquo ; s disease
• 刊名：Bioorganic & Medicinal Chemistry
• 出版年：2017
• 出版时间：15 January 2017
• 年：2017
• 卷：25
• 期：2
• 页码：633-645
• 全文大小：1448 K
• 卷排序：25

文摘

New multifunctional propargylamines were synthesized and evaluated biologically. All compounds selectively inhibit human butyrylcholinesterase. All compounds cross the blood-brain barrier in an in vitro assay. Three compounds also inhibit monamine oxidase B. The crystal structure of human butyrylcholinesterase in complex with 3 was solved.