862423-59-4Relevant academic research and scientific papers
2,4-bis-substituted acetophenone compound, optical isomers and pharmaceutically acceptable salts thereof and application of 2,4-bis-substituted acetophenone compound and optical isomers and pharmaceutically acceptable salts thereof
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Paragraph 0109; 0110; 0111; 0112; 0116; 0117; 0118; 0119, (2017/12/28)
The invention relates to a 2,4-bis-substituted acetophenone compound and optical isomers and pharmaceutically acceptable salts thereof. The invention further discloses an application of the 2,4-bis-substituted acetophenone compound and the optical isomers and pharmaceutically acceptable salts thereof in the aspect of treatment of neural degeneration diseases. The novel compounds have acetylcholinesterase inhibition activity and A beta aggregation inhibiting ability, and hydrolyzates of the novel compounds further have a metal ion chelation action, so that the novel compounds can be used for carrying out treatment from a plurality of targets and have a better application prospect in the treatment of the neural degeneration diseases.
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors
Jia, Ping,Sheng, Rong,Zhang, Jing,Fang, Liang,He, Qiaojun,Yang, Bo,Hu, Yongzhou
body text, p. 772 - 784 (2009/09/05)
A new series of galanthamine derivatives have been designed, synthesized and evaluated as acetylcholinesterase inhibitors. All of the new compounds prepared showed high AChE inhibitory activities, with compound 3e that has an N-hexyl-benzyl piperidine substituent on the nitrogen atom reaching the best inhibitory activity for AChE (IC50 = 5.62 nM). The docking study performed with AutoDock demonstrated that 3e was nicely accommodated by AChE.
Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors
Sheng, Rong,Lin, Xiao,Li, Jingya,Jiang, Yanke,Shang, Zhicai,Hu, Yongzhou
, p. 3834 - 3837 (2007/10/03)
A series of 2-phenoxy-indan-1-one derivatives have been designed, synthesized, and tested as acetylcholinesterase inhibitors. The most potent compound exhibited high AChE inhibitory activity (IC50 = 50 nM), and the molecular docking study indicated that it was nicely accommodated by AChE.
