Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation

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• 作者：Dawid Panek^a ; ¹ ; Anna Więckowska^a ; ¹ ; Tomasz Wichur^a ; Marek Bajda^a ; Justyna Godyń^a ; Jakub Jończyk^a ; Kamil Mika^a ; Jana Janockova^b ; Ondrej Soukup^b ; Damijan Knez^c ; Jan Korabecny^b ; Stanislav Gobec^c ; Barbara Malawska^a ; ^{mfmalaws@cyf-kr.edu.pl}
• 关键词：Alzheimer's disease ; Multifunctional agents ; Acetylcholinesterase inhibitors ; BACE1 inhibitors ; Aβ aggregation ; Molecular docking
• 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：676-695
• 全文大小：1784 K
• 卷排序：125

文摘

Novel multi-target-directed ligands against Alzheimer's disease were designed. Activity against eeAChE, eqBuChE, hBACE1 and Aβ-aggregation was tested. Two derivatives: 26 and 52 with interesting pharmacological profiles were selected.