Báo cáo khoa học: Aromatic amino-acid residues at the active and peripheral anionic sites control the binding of E2020 (AriceptÒ) to cholinesterases
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E2020 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]-methyl)piperidine hydrochloride isa piperidine-based ace-tylcholinesterase (AChE) inhibitor that was approved for the treatment of Alzheimer’s disease in the United States. Structure-activity studiesof thisclassof inhibitorshave indicated that both the benzoyl containing functionality and the N-benzylpiperidine moiety are the key featuresfor binding and inhibition of AChE.
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