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Synthesis and cholinesterase activity of phenylcarbamates related to Rivastigmine, a therapeutic agent for Alzheimer's disease

…, R Ferretti, A Meneguz, MT Volpe, P Lorenzini

文献索引:Mustazza, Carlo; Borioni, Anna; Giudice, Maria Rosaria Del; Gatta, Franco; Ferretti, Rosella; Meneguz, Annarita; Volpe, Maria Teresa; Lorenzini, Paola European Journal of Medicinal Chemistry, 2002 , vol. 37, # 2 p. 91 - 109

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被引用次数: 47

摘要

In order to develop new cholinesterase agents effective against Alzheimer's disease (AD) we synthesized some phenylcarbamates structurally related to Rivastigmine and evaluated their in vitro and in vivo biological activity. Among the compounds which displayed the most significant in vitro activity, 1-[1-(3-dimethylcarbamoyloxyphenyl) ethyl] piperidine (31b), in addition to a simple and cheaper synthesis, showed lower toxicity and very similar ...