Design, synthesis and biological evaluation of novel 1,3 dioxolo 4,5-fisoindolone derivatives / 药学学报
Acta Pharmaceutica Sinica
;
(12): 191-198, 2015.
Article
in Chinese
| WPRIM
| ID: wpr-251796
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.
Full text:
Available
Index:
WPRIM (Western Pacific)
Main subject:
Piperidines
/
Scopolamine
/
Drug Design
/
Chemistry
/
Cholinesterase Inhibitors
/
Inhibitory Concentration 50
/
Dioxoles
/
Drug Therapy
/
Isoindoles
/
Indans
Limits:
Animals
Language:
Chinese
Journal:
Acta Pharmaceutica Sinica
Year:
2015
Type:
Article
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