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Methyl analogues of the experimental Alzheimer drug phenserine: synthesis and structure/activity relationships for acetyl-and butyrylcholinesterase inhibitory action

Q Yu, HW Holloway, JL Flippen-Anderson…

文献索引:Yu; Holloway; Flippen-Anderson; Hoffman; Brossi; Greig Journal of Medicinal Chemistry, 2001 , vol. 44, # 24 p. 4062 - 4071

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被引用次数: 89

摘要

With the goal of developing potential Alzheimer's pharmacotherapeutics, we have synthesized a series of novel analogues of the potent anticholinesterases phenserine (2) and physostigmine (1). These derivatives contain methyl (3, 4, 6), dimethyl (5, 7, 8, 10, 11) and trimethyl (14) substituents in each position of the phenyl group of the phenylcarbamoyl moieties, and with N-methyl and 6-methyl substituents (12, 13, 31, 33). We also quantified ...