Design, synthesis and evaluation of new L-proline derivatives as acetylcholinesterase inhibitors.
- Author:
Yun-feng TIAN
;
Jun-tao CHEN
;
Jun-jie LI
;
Ying-chao ZHANG
;
Ting-ting CAO
;
Zheng-yue MA
- Publication Type:Journal Article
- MeSH:
Acetylcholinesterase;
Cholinesterase Inhibitors;
chemical synthesis;
chemistry;
Drug Design;
Proline;
analogs & derivatives;
Rivastigmine;
chemistry;
Structure-Activity Relationship
- From:
Acta Pharmaceutica Sinica
2015;50(6):719-724
- 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.
