Imidazopyranotacrines as Non-Hepatotoxic, Selective Acetylcholinesterase Inhibitors, and Antioxidant Agents for Alzheimer 1 s Disease Therapy
| Affiliation auteurs | !!!! Error affiliation !!!! |
| Titre | Imidazopyranotacrines as Non-Hepatotoxic, Selective Acetylcholinesterase Inhibitors, and Antioxidant Agents for Alzheimer 1 s Disease Therapy |
| Type de publication | Journal Article |
| Year of Publication | 2016 |
| Auteurs | Boulebd H, Ismaili L, Bartolini M, Bouraiou A, Andrisano V, Martin H, Bonet A, Moraleda I, Iriepa I, Chioua M, Belfaitah A, Marco-Contelles J |
| Journal | MOLECULES |
| Volume | 21 |
| Pagination | 400 |
| Date Published | APR |
| Type of Article | Article |
| Mots-clés | Alzheimer's disease, antioxidant activity, cholinesterase inhibitors, Hepatotoxicity, ORAC, tacrine analogues |
| Résumé | 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 mu M), and a very potent antioxidant agent on the basis of the ORAC test (2.31 +/- 0.29 mu mol.Trolox/mu mol compound). |
| DOI | 10.3390/molecules21040400 |