[Design, synthesis and evaluation of 5-aminobenzimidazolone derivatives as acetylcholinesterase inhibitors].
The target compounds were prepared from 5-aminobenzimidazolone by two steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The AChE inhibitory activity of compound 4d is the best of them, and its IC50 value is equal to 7.2 μmol·L(-1), which is better than that of rivastigmine; moreover the 4d had no inhibitory activities to BuChE. Therefore, the inhibitory activities of 5-aminobenzimidazolone derivatives to acetylcholinesterase are worth further researching.
Zheng-yue
ZY
Ma
Jun-jie
JJ
Li
Jun-tao
JT
Chen
Yun-feng
YF
Tian
Ying-chao
YC
Zhang
Yu-qing
YQ
Cao
D000110:Acetylcholinesterase / Q000378:metabolism; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry*; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry*; D015195:Drug Design; D048448:Phenylcarbamates / Q000737:chemistry; D000068836:Rivastigmine; D013329:Structure-Activity Relationship
D001562:Benzimidazoles; D002800:Cholinesterase Inhibitors; D048448:Phenylcarbamates; D000110:Acetylcholinesterase; D000068836:Rivastigmine