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Design, synthesis and biological evaluation of novel [1,3] dioxolo [4,5-f]isoindolone derivatives

Gong, Y.-X.; Zhu, Q.-F.; Zhong, J.-Q.; Liu, L.-F.; Li, X.-F.; Zheng, X.-H.; Luo, H.-Y.; Zhao, X.-Y.

Yao Xue Xue Bao 50(2): 191-198

2015

ISSN/ISBN: 0513-4870
PMID: 25975027
Document Number: 684240
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.

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