Novel piperidine derivatives. Synthesis and anti-acetylcholinesterase activity of 1-benzyl-4-[2-(N-benzoylamino) ethyl] piperidine derivatives

H Sugimoto, Y Tsuchiya, H Sugumi…

Index: Sugimoto, Hachiro; Tsuchiya, Yutaka; Sugumi, Hiroyuki; Higurashi, Kunizo; Karibe, Norio; et al. Journal of Medicinal Chemistry, 1990 , vol. 33, # 7 p. 1880 - 1887

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Citation Number: 76

Abstract

A series of l-benzy1-4-[2-(N-benzoylamino) ethyl] piperidine derivatives was synthesized and evaluated for antiacetylcholinesterase (anti-AChE) activity. Substituting the benzamide with a bulky moiety in the para position led to a substantial increase in activity. Introduction of an alkyl or phenyl group at the nitrogen atom of benzamide dramatically enhanced the activity. The basic quality of the nitrogen atom of piperidine appears to play an important ...