Design, synthesis and activity of N-acyl-thiochromenothiazol-2-amine as acetylcholinesterase inhibitors.
- Author:
Zheng-Yue MA
;
Yuan-Gong ZHANG
;
Qi YANG
;
Jun-Jie LI
;
Geng-Liang YANG
- Publication Type:Journal Article
- MeSH:
Acetylcholinesterase;
metabolism;
Amines;
chemical synthesis;
pharmacology;
Benzopyrans;
chemical synthesis;
pharmacology;
Cholinesterase Inhibitors;
chemical synthesis;
pharmacology;
Rivastigmine;
Structure-Activity Relationship;
Thiazoles;
chemical synthesis;
pharmacology
- From:
Acta Pharmaceutica Sinica
2014;49(9):1289-1295
- CountryChina
- Language:Chinese
-
Abstract:
A series of novel N-acyl-thiochromenothiazol-2-amine derivatives were designed and synthesized, furthermore, their inhibition effect on acetylcholinesterase was investigated. N-Acyl-thiochromenothiazol-2-amines were prepared from thiophenol 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 10a was the best in them. The IC50 of 10a to AChE is 7.92 μmol x L(-1), and the value is better than that of rivastigmine. N-Acyl-thiochromenothiazol-2-amine derivatives showed a certain bioactivity in vitro, which were worth further investigation.
