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8-Hydroxyquinoline-based anti-Alzheimer multimodal agents
Monatshefte für Chemie - Chemical Monthly ( IF 1.7 ) Pub Date : 2020-07-09 , DOI: 10.1007/s00706-020-02651-0 Damijan Knez , Izidor Sosič , Ana Mitrović , Anja Pišlar , Janko Kos , Stanislav Gobec
中文翻译:
基于8-羟基喹啉的抗阿尔茨海默病多峰剂
更新日期:2020-07-09
Monatshefte für Chemie - Chemical Monthly ( IF 1.7 ) Pub Date : 2020-07-09 , DOI: 10.1007/s00706-020-02651-0 Damijan Knez , Izidor Sosič , Ana Mitrović , Anja Pišlar , Janko Kos , Stanislav Gobec
Abstract
The concept of multitarget-directed ligands (MTDLs) has attracted considerable interest in the development of agents against Alzheimer’s disease. Cathepsin B, a cysteine protease, and butyrylcholinesterase, a serine hydrolase, play important function in the development and progression of Alzheimer’s disease. We present herein the evaluation of 8-hydroxyquinoline-based analogues with activities against butyrylcholinesterase and β-secretase activity of cathepsin B. Furthermore, inhibition of amyloid β aggregation, chelation of copper and zinc ions coupled with antioxidative properties and safe cytotoxicity profile of (1R,2S)-N-ethyl-2-[[(8-hydroxy-5-nitroquinolin-7-yl)methyl]amino]cyclohexane-1-carboxamide suggest that this derivative is a good starting point for optimization towards an effective multifunctional ligand.Graphic abstract
中文翻译:
基于8-羟基喹啉的抗阿尔茨海默病多峰剂