Design, synthesis and evaluation of 5-aminobenzimidazolone derivatives as acetylcholinesterase inhibitors / 药学学报
Acta Pharmaceutica Sinica
;
(12): 64-69, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-251816
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Acetylcholinesterase
/
Structure-Activity Relationship
/
Benzimidazoles
/
Drug Design
/
Chemistry
/
Cholinesterase Inhibitors
/
Phenylcarbamates
/
Rivastigmine
/
Metabolism
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2015
Type:
Article
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