Design, synthesis and biological evaluation of novel 1,3dioxolo4,5-fisoindolone derivatives

A series of 1,3dioxolo4,5-fisoindolone 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 �mol·L^-1) and I₂ (IC₅₀ value of 0.080 �mol·L^-1) showed the strongest AChE inhibitory activity, which are equipotent to donepezil (IC₅₀ value of 0.094 �mol·L^-1). Moreover, compounds I₁-I₄ could improve the memory impairment induced by scopolamine in mice.