title: [Design, synthesis and biological evaluation of novel [1,3] dioxolo [4,5-f]isoindolone derivatives].
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.
authors.forename: Yong-Xiang
authors.initials: YX
authors.lastname: Gong
authors.forename: Qi-Feng
authors.initials: QF
authors.lastname: Zhu
authors.forename: Jin-Qing
authors.initials: JQ
authors.lastname: Zhong
authors.forename: Li-Fei
authors.initials: LF
authors.lastname: Liu
authors.forename: Xu-Fei
authors.initials: XF
authors.lastname: Li
authors.forename: Xiao-He
authors.initials: XH
authors.lastname: Zheng
authors.forename: Hong-Ying
authors.initials: HY
authors.lastname: Luo
authors.forename: Xu-Yang
authors.initials: XY
authors.lastname: Zhao
mesh_terms: D000818:Animals; D002800:Cholinesterase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry*; D004149:Dioxoles / Q000138:chemical synthesis* / Q000737:chemistry; D000077265:Donepezil; D015195:Drug Design; D007189:Indans; D020128:Inhibitory Concentration 50; D054833:Isoindoles / Q000138:chemical synthesis* / Q000737:chemistry*; D008569:Memory Disorders / Q000188:drug therapy; D051379:Mice; D010880:Piperidines; D012601:Scopolamine
chemical_list: D002800:Cholinesterase Inhibitors; D004149:Dioxoles; D007189:Indans; C110621:Isoindol-1-one; D054833:Isoindoles; D010880:Piperidines; D000077265:Donepezil; D012601:Scopolamine