A series of imine resveratrol derivatives (1-20) have been designed, synthesized, and evaluated as multi-targeted compounds for the treatment of Alzheimer's disease (AD). In vitro studies show that most of the molecules exhibit a significant ability to inhibit self-induced and Cu(2+)-induced β-amyloid (Aβ₁₋₄₂) aggregation, and to function as potential antioxidants and biometal chelators. In particular, compound 9 is a potential lead compound for AD treatment (for compound 9, IC₅₀ = 14.1 μM for the antioxidant activity using DPPH free radical method; 64.6% at 20 μM for self-induced Aβ aggregation). Moreover, it is capable of decreasing reactive oxygen species (ROS) induced by Cu-Aβ and shows good neuroprotective effects in human SH-SY5Y neuroblastoma cells. Taken together, these results suggest that 9 might be a promising lead compound for AD treatment.
Keywords: Alzheimer's disease; Antioxidant; BSVVLXIGPDFSEZ-RIYZIHGNSA-N; CHBGIQHEGBKNGA-NTEUORMPSA-N; COFLOZFCNFCJFM-OQLLNIDSSA-N; CPOKOAWVSUHOCZ-MHWRWJLKSA-N; CXQBWMKQSJPURB-XNTDXEJSSA-N; DTKVTDFIUFYZDW-OQLLNIDSSA-N; GJZBNSJPZKCNPU-LFIBNONCSA-N; GRWIZXASAOKOEZ-GXDHUFHOSA-N; IUPUQXNVHRUSEI-OQLLNIDSSA-N; IWCJTSCDZDXKBK-OQLLNIDSSA-N; KILNMRJUXROOCU-NTEUORMPSA-N; Metal chelator; Neuroprotection; OZUBFLPYRPJKQL-XNTDXEJSSA-N; POLJRSQMPKDDIY-NTEUORMPSA-N; PQKMAPANQMNEHB-NTEUORMPSA-N; QIYHCQVVYSSDTI-GXDHUFHOSA-N; Resveratrol derivatives; SDHKTTFTBJGDQX-OQLLNIDSSA-N; UALRWOGQNILXLJ-NTEUORMPSA-N; USHSXCMBQPJHEF-OQLLNIDSSA-N; VISLUSLXCVLVTQ-RIYZIHGNSA-N; ZUHWLAWLODQICJ-OQLLNIDSSA-N; β-Amyloid aggregation.
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