Flexible 1-[(2-aminoethoxy) alkyl]-3-ar (o) yl (thio) ureas as novel acetylcholinesterase inhibitors. Synthesis and biochemical evaluation

…, F Calmel, DCH Bigg, E Carilla, M Briley

Index: Vidaluc; Calmel; Bigg; Carilla; Briley Journal of Medicinal Chemistry, 1995 , vol. 38, # 15 p. 2969 - 2973

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Citation Number: 12

Abstract

A series of flexible l-(2-aminoethoxy)-3-ar (o) yl (thio) ureas was synthesized and assessed for antiacetylcholinesterase activity. This series was designed in order to optimize the spacer length linking the two pharmacophoric moieties, ie, the basic nitrogen and the ar (o) yl (thio)- urea unit, and to test compounds with greater conformational flexibility. Thus, the replacement of the previously described spacer, 4-piperidinylethyl, by a linear ethoxyethyl ...