Design, synthesis and biological evaluation of novel 1,3 dioxolo 4,5-fisoindolone derivatives.
- Author:
Yong-Xiang GONG
;
Qi-Feng ZHU
;
Jin-Qing ZHONG
;
Li-Fei LIU
;
Xu-Fei LI
;
Xiao-He ZHENG
;
Hong-Ying LUO
;
Xu-Yang ZHAO
- Publication Type:Journal Article
- MeSH:
Animals;
Cholinesterase Inhibitors;
chemical synthesis;
chemistry;
Dioxoles;
chemical synthesis;
chemistry;
Drug Design;
Indans;
Inhibitory Concentration 50;
Isoindoles;
chemical synthesis;
chemistry;
Memory Disorders;
drug therapy;
Mice;
Piperidines;
Scopolamine Hydrobromide
- From:
Acta Pharmaceutica Sinica
2015;50(2):191-198
- 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.
