Design, synthesis and evaluation of N-acyl-4-phenylthiazole-2-amines as acetylcholinesterase inhibitors.
- Author:
Zheng-Yue MA
;
Qi YANG
;
Yuan-Gong ZHANG
;
Jun-Jie LI
;
Geng-Liang YANG
- Publication Type:Journal Article
- MeSH:
Acetylcholinesterase;
metabolism;
Alkaloids;
pharmacology;
Amines;
chemical synthesis;
pharmacology;
Cholinesterase Inhibitors;
chemical synthesis;
pharmacology;
Drug Design;
Rivastigmine;
pharmacology;
Sesquiterpenes;
pharmacology;
Structure-Activity Relationship;
Thiazoles;
pharmacology
- From:
Acta Pharmaceutica Sinica
2014;49(6):813-818
- CountryChina
- Language:Chinese
-
Abstract:
N-Acyl-4-phenylthiazole-2-amines were designed and synthesized, moreover their effects on acetylcholinesterase activities were tested. N-Acyl-4-phenylthiazole-2-amines were prepared from substituted 2-bromo-1-acetophenones by three steps reaction, and their AChE inhibitory activities were measured by Ellman method in vitro. The results showed that the target compounds had a certain inhibitory activity on AChE in vitro. Among them, 8c was the best, and IC50 of 8c was 0.51 micromol x L(-1), better than that of rivastigmine and Huperzine-A. The inhibitory activities of N-acyl-4-phenylthiazole-2-amines on acetylcholinesterase are worth while to be further studied.
