Spirovesamicols: conformationally restricted analogs of 2-(4-phenylpiperidino) cyclohexanol (vesamicol, AH5183) as potential modulators of presynaptic cholinergic …

…, C Foulon, SK Akella, SM Parsons

Index: Efange; Khare; Foulon; Akella; Parsons Journal of Medicinal Chemistry, 1994 , vol. 37, # 16 p. 2574 - 2582

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Citation Number: 42

Abstract

In an effort to develop selective inhibitors of vesicular acetylcholine storage, we have synthesized a series of semirigid vesamicol receptor ligands based on the structure of 2-(4- phenylpiperidino)-cyclohexanol (vesamicol, AH5183, 1). In these compounds, the planes of the phenyl and piperidyl moieties of the parent ligand 1 are held at right angles by vinyl, ethylene, and propylene bridges to form N-substituted derivatives of spiro [indene-1,#- ...