Repurposing N,N'-bis-(arylamidino)-1,4-piperazinedicarboxamidines: An unexpected class of potent inhibitors of cholinesterases

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• 作者：Anne Loesche^a ; ¹ ; Jana Wiese^a ; ¹ ; Sven Sommerwerk^a ; Vivienne Simon^a ; Wolfgang Brandt^b ; René ; Csuk^a ; ^{rene.csuk@chemie.uni-halle.de}
• 关键词：Picloxydine ; Acetylcholinesterase ; Butyrylcholinesterase ; Bisbiguanides
• 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：430-434
• 全文大小：895 K
• 卷排序：125

文摘

Twenty one analogs of the antiseptic agent picloxydine were synthesized. They were screened for their ability to inhibit cholinesterases AChE and BChE. A p-nitro substituted bisbiguanide 43 was a good inhibitor for AChE. A p-tert-butyl substituted analog 42, however, inhibited BChE in the low μM range.