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Synthesis,antioxidant and Aβ anti-aggregation properties of new ferulic,caffeic and lipoic acid derivatives obtained by the Ugi four-component reaction
Institution:1. Department of Clinical and Experimental Medicine, University of Parma, Parma, Italy;2. Department of Medicine, University of Perugia, Perugia, Italy;3. Clinical Research Branch, National Institute on Aging, National Institutes of Health, Baltimore, MD, United States;4. Laboratory of Clinical Chemistry and Hematology, University Hospital of Parma, Parma, Italy;5. Department of Medical Sciences, Uppsala University, Uppsala, Sweden;6. Department of Public Health and Caring Sciences, Uppsala University, Uppsala, Sweden
Abstract:We report herein the synthesis antioxidant and Aβ anti-aggregation capacity of (E)-N-benzyl-N-2-(benzylamino)-2-oxoethyl]-3-(aryl)acrylamides and related (R)-N-benzyl-N-(2-(benzylamino)-2-oxoethyl)-5-(1,2-dithiolan-3-yl)pentanamides 112. These compounds have been obtained, via Ugi four-component reaction, from modest to good yields. Their antioxidant analysis, using the DPPH and ORAC assays, allowed us to identify compounds 8 and 9, as potent antioxidant agents, showing also strong Aβ1–40 self-aggregation inhibition, two biological properties of interest in pathologies linked to the oxidative stress, such as Alzheimer’s disease.
Keywords:Antioxidants  Benzylamine  Benzyl isocyanide  Caffeic acid  Ferulic acid  Multicomponent reactions  Ugi four-component reaction
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