imidazopyranotacrines as non-hepatotoxic, selective acetylcholinesterase inhibitors, and antioxidant agents for alzheimer′s disease therapy
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2016
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Abstract
Herein we describe the synthesis and in vitro biological evaluation of thirteen new, racemic, diversely functionalized imidazo pyranotacrines as non-hepatotoxic, multipotent tacrine analogues. Among these compounds, 1-(5-amino-2-methyl-4-(1-methyl-1H-imidazol-2-yl)-6,7,8,9-tetrahydro-4H-pyrano[2,3-b]quinolin-3-yl)ethan-1-one (4) is non-hepatotoxic (cell viability assay on HepG2 cells), a selective but moderately potent EeAChE inhibitor (IC50 = 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).
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boulebd2016moleculesimidazopyranotacrines
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| Authors | ;Houssem Boulebd;Lhassane Ismaili;Manuela Bartolini;Abdelmalek Bouraiou;Vincenza Andrisano;Helene Martin;Alexandre Bonet;Ignacio Moraleda;Isabel Iriepa;Mourad Chioua;Ali Belfaitah;José Marco-Contelles |
| Journal | Journal of ethnopharmacology |
| Year | 2016 |
| DOI |
10.3390/molecules21040400
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