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 ; akup>aup> ; Damijan Knezup>aup> ; Nicolas Coquelleup>bup> ; Boris Brusup>aup> ; Anja Pi&scaron ; larup>aup> ; Florian Nachonup>cup> ; Xavier Brazzolottoup>cup> ; Janko Kosup>aup> ; Jacques-Philippe Colletierup>bup> ; Stanislav Gobecup>aup>up> ; up>up>stanislav.gobec@ffa.uni-lj.siup>
• 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.