Design, synthesis, and evaluation of 2-phenoxy-indan-1-one derivatives as acetylcholinesterase inhibitors.
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.
Sheng
Rong
R
ZJU-ENS Joint Laboratory of Medicinal Chemistry, Zhejiang University, Hubin Campus, Hangzhou 310031,China.
Lin
Xiao
X
Li
Jingya
J
Jiang
Yanke
Y
Shang
Zhicai
Z
Hu
Yongzhou
Y
D000110:Acetylcholinesterase / Q000737:chemistry; D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D015195:Drug Design; D007189:Indans / Q000138:chemical synthesis* / Q000494:pharmacology; D020128:Inhibitory Concentration 50; D007659:Ketones; D008958:Models, Molecular; D011485:Protein Binding; D051381:Rats; D013329:Structure-Activity Relationship
D002800:Cholinesterase Inhibitors; D007189:Indans; D007659:Ketones; D000110:Acetylcholinesterase