Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease

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• 作者：Jakub Jeř&aacute ; bek^a ; ^b ; Elisa Uliassi^a ; Laura Guidotti^a ; Jan Kor&aacute ; bečný ; ^c ; ^d ; Ondřej Soukup^c ; ^d ; Vendula Sepsova^e ; Martina Hrabinova^e ; Kamil Kuča^c ; ^d ; Manuela Bartolini^a ; Luis Emiliano Peñ ; a-Altamira^a ; Sabrina Petralla^a ; Barbara Monti^a ; Marinella Roberti^a ; ^{marinella.roberti@unibo.it} ; Maria Laura Bolognesi^a ; ^{marialaura.bolognesi@unibo.it}
• 关键词：Alzheimer's disease ; Amyloid ; Acetylcholinesterase ; Multitarget compounds ; Neuroinflammation
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：127
• 期：Complete
• 页码：250-262
• 全文大小：1450 K
• 卷排序：127

文摘

Novel multitarget ligands against Alzheimer's disease have been developed. The new hybrids have been obtained by fusing tacrines with resveratrol. The most interesting hybrids inhibited hAChE and modulated Aβ self-aggregation. Hybrid 12 showed a low neurotoxicity and neuroprotective effect on neuroinflammation.