Design, synthesis and evaluation of new acetylcholinesterase inhibitors.
- Author:
Zheng-Yue MA
;
Yuan-Gong ZHANG
;
Qi YANG
;
Jun-Jie LI
;
Geng-Liang YANG
- Publication Type:Journal Article
- MeSH:
Acetylcholinesterase;
metabolism;
Cholinesterase Inhibitors;
chemical synthesis;
chemistry;
pharmacology;
Drug Design;
Inhibitory Concentration 50;
Molecular Structure;
Thiazoles;
chemical synthesis;
chemistry;
pharmacology
- From:
Acta Pharmaceutica Sinica
2014;49(3):346-351
- CountryChina
- Language:Chinese
-
Abstract:
A series of novel 2-amino-4-phenylthiazole derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase were investigated. 2-Amino-4-phenylthiazoles were prepared from alpha-bromoacetophenones by Hantzsch reaction, acylation reaction and substitution reaction. Moreover, their bioactivities as AChE inhibitors in vitro were measured with Ellman spectrophotometry. The results showed that most of them had a certain inhibition activity on AChE, and the compound 8a was the best of them. The IC50 of 8a to AChE is 3.54 micromol x L(-1), and the value was better than that of rivastigmine. 2-Amino-4-phenylthiazole derivatives showed a certain bioactivity in vitro, which were worth further investigation.
