Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy

详细信息    查看全文

• 作者：Youssef Dgachi^a ; Olga Sokolov^b ; Vincent Luzet^b ; Justyna Godyń^c ; Dawid Panek^c ; Alexandre Bonet^d ; Hé ; lè ; ne Martin^d ; Isabel Iriepa^e ; Ignacio Moraleda^e ; Cristina Garcí ; a-Iriepa^f ; Jana Janockova^g ; Lysiane Richert^d ; Ondrej Soukup^g ; Barbara Malawska^c ; Fakher Chabchoub^a ; ^{fakher.chabchoub@yahoo.fr} ; José ; Marco-Contelles^h ; ^{iqoc21@iqog.csic.es} ; Lhassane Ismaili^b ; ^{lhassane.ismaili@univ-fcomte.fr}
• 关键词：Alzheimer's disease ; Acetylcholinesterase inhibitors ; Antioxidants ; Hepatotoxicity ; Brain blood barrier ; Molecular modeling ; Multifunctional agents
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：27 January 2017
• 年：2017
• 卷：126
• 期：Complete
• 页码：576-589
• 全文大小：1796 K
• 卷排序：126

文摘

12 novel multitarget directed ligands for Alzheimer's disease. The in vitro enzymatic and hepatotoxic activities were evaluated. The primary structure–activity relationships were discussed. Compound 2h is non-hepatotoxic, and selective hAChE inhibitor.