Synthesis and structure-activity relationships of acetylcholinesterase inhibitors: 1-benzyl-4-[(5, 6-dimethoxy-1-oxoindan-2-yl) methyl] piperidine hydrochloride and …

H Sugimoto, Y Iimura, Y Yamanishi…

Index: Sugimoto; Iimura; Yamanishi; Yamatsu Journal of Medicinal Chemistry, 1995 , vol. 38, # 24 p. 4821 - 4829

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Citation Number: 266

Abstract

Following the discovery of a new series of anti-acetylcholinesterase (anti-AChE) inhibitors such as 1-benzyl-4-[2-(N-benzoylamino) ethyl] piperidine (l), we reported that its rigid analogue, 1-benzyl-4-(2-isoindolin-2-ylethyl) piperidine (51, had more potent activity. We have extended the structure-activity relationship (SAR) study for the rigid analogue and found that the 2-isoindoline moiety in compound 5 can be replaced with a indanone ...