Design, synthesis and evaluation of new L-phenylalanine derivatives as acetylcholinesterase inhibitors / 中国药学杂志
Chinese Pharmaceutical Journal
;
(24): 1180-1185, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-859555
ABSTRACT
OBJECTIVE:
To research the effect of new L-phenylalanine derivatives on acetylcholinesterase (AChE) activity.METHODS:
New L-phenylalanine derivatives were synthesized from substituted 2-bromo-l-acetophenones by four steps reaction, and their inhibitory activities on AChE were measured by Ellman method in vitro.RESULTS:
The evaluation results showed that most derivatives possessed AChE inhibitory effect and the activity of compound 8b was the most potent with an IC50 value of 8.73 × 10-6 mol · L-1, which was more potent than that of rivastigmine; moreover, compound 8b had no inhibitory activities to BuChE.CONCLUSION:
The inhibitory activities of new L-phenylalanine derivatives on acetylcholinesterase are worth studying further.
Full text:
Available
Index:
WPRIM (Western Pacific)
Language:
Chinese
Journal:
Chinese Pharmaceutical Journal
Year:
2015
Type:
Article
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