Design, synthesis and evaluation of new L-proline derivatives as acetylcholinesterase inhibitors.
- Author:
Yunfeng TIAN
;
Juntao CHEN
;
Junjie LI
;
Yingchao ZHANG
;
Tingting CAO
;
Zhengyue MA
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2015;50(6):719-24
- CountryChina
- Language:Chinese
-
Abstract:
In this paper, fourteen new L-proline derivatives were designed and synthesized, and their acetlcholinesterase (AChE) inhibitory activities were also investigated in vitro. New L-proline derivatives were prepared from substituted 2-bromo-1-acetophenones through four-step reaction; and their bioactivities as AChE inhibitors were measured by Ellman spectrophotometry. The results showed that the target compounds had a certain AChE inhibitory activity to in vitro. The bioactivity of compound 8b was the best of them, and its IC50 value was 5.45 µmol.L-1, which was better than that of rivastigmine. So the acetylcholinesterase inhibitory activities of new L-proline derivatives were worth to be further studied.
