Toward a Rational Design of Multitarget-Directed Antioxidants: Merging Memoquin and Lipoic Acid Molecular Frameworks

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• 作者：Maria Laura Bolognesi ; Andrea Cavalli ; Christian Bergamini ; Romana Fato ; Giorgio Lenaz ; Michela Rosini ; Manuela Bartolini ; Vincenza Andrisano ; Carlo Melchiorre
• 刊名：Journal of Medicinal Chemistry
• 出版年：2009
• 出版时间：December 10, 2009
• 年：2009
• 卷：52
• 期：23
• 页码：7883-7886
• 全文大小：755K
• 年卷期：v.52,no.23(December 10, 2009)
• ISSN：1520-4804

文摘

Novel multitargeted antioxidants 3−6 were designed by combining the antioxidant features, namely, a benzoquinone fragment and a lipoyl function, of two multifunctional lead candidates. They were then evaluated to determine their profile against Alzheimer’s disease. They showed antioxidant activity, improved following enzymatic reduction, in mitochondria and T67 cell line. They also displayed a balanced inhibitory profile against amyloid-β aggregation and acetylcholinesterase, emerging as promising molecules for neuroprotectant lead discovery.