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Title

Imidazopyranotacrines as Non-Hepatotoxic, Selective Acetylcholinesterase Inhibitors, and Antioxidant Agents for Alzheimer's Disease Therapy

AuthorsBoulebd, Houssem; Ismaili, L.; Bartolini, Manuela; Bouraiou, Abdelmalek; Andrisano, Vincenza; Martin, Hélène; Bonet, Alexandre; Moraleda, Ignacio; Iriepa, Isabel; Chioua, Mourad ; Belfaitah, Ali; Marco-Contelles, José
Issue Date24-Mar-2016
PublisherMultidisciplinary Digital Publishing Institute
CitationMolecules 21 (4): 400 (2016)
AbstractHerein we describe the synthesis and <i>in vitro</i> biological evaluation of thirteen new, racemic, diversely functionalized <i>imidazo pyranotacrines</i> as non-hepatotoxic, multipotent tacrine analogues. Among these compounds, 1-(5-amino-2-methyl-4-(1-methyl-1<i>H</i>-imidazol-2-yl)-6,7,8,9-tetrahydro-4<i>H</i>-pyrano[2,3-<i>b</i>]quinolin-3-yl)ethan-1-one (4) is non-hepatotoxic (cell viability assay on HepG2 cells), a selective but moderately potent <i>Ee</i>AChE inhibitor (IC<sub>50</sub> = 38.7 ± 1.7 μM), and a very potent antioxidant agent on the basis of the ORAC test (2.31 ± 0.29 μmol·Trolox/μmol compound).
Publisher version (URL)http://doi.org/10.3390/molecules21040400
URIhttp://hdl.handle.net/10261/149195
DOI10.3390/molecules21040400
Identifiersdoi: 10.3390/molecules21040400
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