کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1396045 | 1501170 | 2011 | 9 صفحه PDF | دانلود رایگان |
A series of 9-N-substituted berberine derivatives were synthesized and biologically evaluated as antioxidant and inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase and amyloid-β aggregation. Most of these compounds exhibited very good antioxidant activities, inhibitive activities of AChE and amyloid-β aggregation. Among them, compound 8d, (o-methylphenethyl)amino linked at the 9-position of berberine, was found to be a good antioxidant (with 4.05 μM of Trolox equivalents), potent inhibitor of AChE (an IC50 value of 0.027 μM), and high active inhibitor of amyloid-β aggregation (an IC50 value of 2.73 μM).
A series of 9-N-substituted berberine derivatives were synthesized and biologically evaluated as antioxidant and inhibitors of acetylcholinesterase (AChE), butyrylcholinesterase and amyloid-β aggregation.Figure optionsDownload as PowerPoint slideHighlights
► 24 9-N substituted berberine derivatives, as multi-functional anti-Alzheimer agents were synthesized.
► Most of the compounds showed high inhibitory activities for AChE and BuChE.
► All the compounds exhibited high potent antioxidation activity.
► Some of these compounds exhibited high inhibitory activities of self-induced Aβ aggregation.
Journal: European Journal of Medicinal Chemistry - Volume 46, Issue 12, December 2011, Pages 5885–5893