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Synthesis of alkylene linked bis-THA and alkylene linked benzyl-THA ashighly potent and selective inhibitors and molecular probes ofacetylcholinesterase

…, F Hong, P Quiram, T Jelacic, S Brimijoin

文献索引:Pang, Yuan-Ping; Hong, Feng; Quiram, Polly; Jelacic, Tanya; Brimijoin, Stephen Journal of the Chemical Society - Perkin Transactions 1, 1997 , # 2 p. 171 - 176

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被引用次数: 41

摘要

An efficient and economical synthesis of a series of rationally designed novel 9, 9′-(alkane- 1, ω-diyldiimino)-1, 2, 3, 4-tetrahydroacridines (ω= 7–10) and a second series of new analogues, 9-(ω-phenylalkylamino)-1, 2, 3, 4-tetrahydroacridines (ω= 4–10), is reported. Compounds in the first series are found to be up to 10 000-fold more selective and 1000-fold more potent in reversibly inhibiting rat acetylcholinesterase (AChE) than the monomer, 9- ...