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[Design, synthesis and biological evaluation of novel [1,3] dioxolo [4,5-f]isoindolone derivatives].
- Source :
-
Yao xue xue bao = Acta pharmaceutica Sinica [Yao Xue Xue Bao] 2015 Feb; Vol. 50 (2), pp. 191-8. - Publication Year :
- 2015
-
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.
- Subjects :
- Animals
Cholinesterase Inhibitors chemical synthesis
Dioxoles chemistry
Donepezil
Indans
Inhibitory Concentration 50
Memory Disorders drug therapy
Mice
Piperidines
Scopolamine
Cholinesterase Inhibitors chemistry
Dioxoles chemical synthesis
Drug Design
Isoindoles chemical synthesis
Isoindoles chemistry
Subjects
Details
- Language :
- Chinese
- ISSN :
- 0513-4870
- Volume :
- 50
- Issue :
- 2
- Database :
- MEDLINE
- Journal :
- Yao xue xue bao = Acta pharmaceutica Sinica
- Publication Type :
- Academic Journal
- Accession number :
- 25975027