Article
Aromatic amino-acid residues at the active and peripheral anionic sites control the binding of E2020 (Aricept) to cholinesterases.
European journal of biochemistry - 1 Nov 2003
Saxena Ashima, Fedorko James M, Vinayaka C R, Medhekar Rohit, Radić Zoran, Taylor Palmer, Lockridge Oksana, Doctor Bhupendra P
Abstract excerpt
E2020 (R,S)-1-benzyl-4-[(5,6-dimethoxy-1-indanon)-2-yl]methyl)piperidine hydrochloride is a piperidine-based acetylcholinesterase (AChE) inhibitor that was approved for the treatment of Alzheimer's disease in the United States. Structure-activity studies of this class of inhibitors have indicated that both the benzoyl containing functionality and the N-benzylpiperidine moiety are the key features for binding and...
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