Design, synthesis and evaluation of 5-aminobenzimidazolone derivatives as acetylcholinesterase inhibitors.
- Author:
Zheng-yue MA
;
Jun-jie LI
;
Jun-tao CHEN
;
Yun-feng TIAN
;
Ying-chao ZHANG
;
Yu-qing CAO
- Publication Type:Journal Article
- MeSH:
Acetylcholinesterase;
metabolism;
Benzimidazoles;
chemical synthesis;
chemistry;
Cholinesterase Inhibitors;
chemical synthesis;
chemistry;
Drug Design;
Phenylcarbamates;
chemistry;
Rivastigmine;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2015;50(1):64-69
- CountryChina
- Language:Chinese
-
Abstract:
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.
