Imidazopyranotacrines as Non-Hepatotoxic, Selective Acetylcholinesterase Inhibitors, and Antioxidant Agents for Alzheimer′s Disease Therapy
oleh: 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
| Format: | Article |
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| Diterbitkan: | MDPI AG 2016-03-01 |
Deskripsi
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).