Design, synthesis and evaluation of galanthamine derivatives as acetylcholinesterase inhibitors.
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 (IC(50)=5.62 nM). The docking study performed with AutoDock demonstrated that 3e was nicely accommodated by AChE.
ZJU-ENS Joint Laboratory of Medicinal Chemistry, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, China.
Ping
P
Jia
Rong
R
Sheng
Jing
J
Zhang
Liang
L
Fang
Qiaojun
Q
He
Bo
B
Yang
Yongzhou
Y
Hu
D000818:Animals; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis*; D003198:Computer Simulation; D015195:Drug Design; D005702:Galantamine / Q000138:chemical synthesis* / Q000494:pharmacology; D006801:Humans; D020128:Inhibitory Concentration 50; D010880:Piperidines; D011485:Protein Binding; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D010880:Piperidines; D005702:Galantamine