913380-93-5Relevant academic research and scientific papers
Design, synthesis and evaluation of difunctionalized 4-hydroxybenzaldehyde derivatives as novel cholinesterase inhibitors
Yu, Liang,Cao, Rihui,Yi, Wei,Yan, Qin,Chen, Zhiyong,Ma, Lin,Song, Huacan
experimental part, p. 1216 - 1220 (2010/11/18)
A series of difunctionalized 4-hydroxybenzaldehyde derivatives were designed, synthesized and evaluated as cholinesterase (acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)) inhibitors. The results demonstrated that all the compounds had more potent AChE and BChE inhibitory activities than galanthamine-HBr, one of the best cholinesterase inhibitors known so far. The inhibition mechanism revealed that the best active compound 4e displayed a mix-type mode of AChE and BChE by its dual-site interactions with the catalytic triad active center and the peripheral anionic site (PAS) of enzyme. All these data suggested that further development of such compounds may be of interest.
Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors
Jia, Ping,Sheng, Rong,Zhang, Jing,Fang, Liang,He, Qiaojun,Yang, Bo,Hu, Yongzhou
experimental part, 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.
