Design, synthesis and biological evaluation of novel 1,3 dioxolo 4,5-fisoindolone derivatives.
- Author:
Yongxiang GONG
;
Qifeng ZHU
;
Jinqing ZHONG
;
Lifei LIU
;
Xufei LI
;
Xiaohe ZHENG
;
Hongying LUO
;
Xuyang ZHAO
- Publication Type:Journal Article
- From:
Acta Pharmaceutica Sinica
2015;50(2):191-8
- CountryChina
- Language:Chinese
-
Abstract:
A series of [1,3]dioxolo[4,5-f]isoindolone derivatives were designed, synthesized and evaluated as inhibitors of acetylcholinesterases (AChE). Furthermore, their effects on memory impairment of mice induced by scopolamine were investigated with step-through test. The results suggested that most of the target compounds exhibited potential inhibition on AChE with IC50 values at micromolar range. Compounds I1 (IC50 value of 0.086 μmol · L(-1)) and I2 (IC50 value of 0.080 μmol · L(-1)) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC50 value of 0.094 μmol · L(-1)). Moreover, compounds I1-I4 could improve the memory impairment induced by scopolamine in mice.
