Paper Report for: Hu_2019_J.Enzyme.Inhib.Med.Chem_34_1083
Reference
Title: Synthesis and biological evaluation of 3-(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer's disease agents Hu YH, Yang J, Zhang Y, Liu KC, Liu T, Sun J, Wang XJ Ref: J Enzyme Inhib Med Chem, 34:1083, 2019 : PubMed
The work is focused on the design of drugs that prevent and treat Alzheimer's disease (AD) and its complications. A series of 3-(4-aminophenyl)-coumarin derivatives designed, synthesised, fully characterised and evaluated in vitro/vivo. The biological assay experiments showed that some compounds displayed a clearly selective inhibition for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). Among all compounds, compound 4m exhibited the highest AChE inhibition with an IC50 value of 0.091 +/- 0.011 microM and compound 4k exhibited the highest BuChE inhibition with an IC50 value of 0.559 +/- 0.017 microM. A zebrafish behaviour analyser (Zebrobox) was used to determine the behavioural effects of the active compound on the movement distance of the aluminium chloride-induced zebrafish. Compound 4m offered a potential drug design concept for the development of therapeutic or preventive agents for AD and its complications.
        
Related information
Citations formats
Hu YH, Yang J, Zhang Y, Liu KC, Liu T, Sun J, Wang XJ (2019) Synthesis and biological evaluation of 3-(4-aminophenyl)-coumarin derivatives as potential anti-Alzheimer's disease agents J Enzyme Inhib Med Chem34: 1083-1092
Hu YH, Yang J, Zhang Y, Liu KC, Liu T, Sun J, Wang XJ (2019) J Enzyme Inhib Med Chem34: 1083-1092