| Title : Imidazopyranotacrines as Non-Hepatotoxic, Selective Acetylcholinesterase Inhibitors, and Antioxidant Agents for Alzheimer's Disease Therapy - Boulebd_2016_Molecules_21_ |
| Author(s) : 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 |
| Ref : Molecules , 21 : , 2016 |
|
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 muM), and a very potent antioxidant agent on the basis of the ORAC test (2.31 +/- 0.29 mumol.Trolox/mumol compound). |
| PubMedSearch : Boulebd_2016_Molecules_21_ |
| PubMedID: 27023499 |
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 (2016)
Imidazopyranotacrines as Non-Hepatotoxic, Selective Acetylcholinesterase Inhibitors, and Antioxidant Agents for Alzheimer's Disease Therapy
Molecules
21 :
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 (2016)
Molecules
21 :