| Title : Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy - Dgachi_2016_Eur.J.Med.Chem_126_576 |
| Author(s) : Dgachi Y , Sokolov O , Luzet V , Godyn J , Panek D , Bonet A , Martin H , Iriepa I , Moraleda I , Garcia-Iriepa C , Janockova J , Richert L , Soukup O , Malawska B , Chabchoub F , Marco-Contelles J , Ismaili L |
| Ref : Eur Journal of Medicinal Chemistry , 126 :576 , 2016 |
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Abstract :
Herein we report an efficient two step synthesis and biological assessment of 12 racemic tetrahydropyranodiquinolin-8-amines derivatives as antioxidant, cholinesterase inhibitors and non-hepatotoxic agents. Based on the results of the primary screening, we identified 7-(3-methoxyphenyl)-9,10,11,12-tetrahydro-7H-pyrano[2,3-b:5,6-h']diquinolin-8-ami ne (2h) as a particularly interesting non-hepatotoxic compound that shows moderate antioxidant activity (1.83 equiv Trolox in the ORAC assay), a non competitive inhibition of hAChE (IC50 = 0.75 +/- 0.01 muM), and brain permeable as determined by the PAMPA-Blood Brain Barrier assay. |
| PubMedSearch : Dgachi_2016_Eur.J.Med.Chem_126_576 |
| PubMedID: 27918993 |
Dgachi Y, Sokolov O, Luzet V, Godyn J, Panek D, Bonet A, Martin H, Iriepa I, Moraleda I, Garcia-Iriepa C, Janockova J, Richert L, Soukup O, Malawska B, Chabchoub F, Marco-Contelles J, Ismaili L (2016)
Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy
Eur Journal of Medicinal Chemistry
126 :576
Dgachi Y, Sokolov O, Luzet V, Godyn J, Panek D, Bonet A, Martin H, Iriepa I, Moraleda I, Garcia-Iriepa C, Janockova J, Richert L, Soukup O, Malawska B, Chabchoub F, Marco-Contelles J, Ismaili L (2016)
Eur Journal of Medicinal Chemistry
126 :576