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ID: ALA1152530

Journal: Bioorg Med Chem

Title: Fluorinated pyridinium oximes as potential reactivators for acetylcholinesterases inhibited by paraoxon organophosphorus agent.

Authors: Jeong HC, Park NJ, Chae CH, Musilek K, Kassa J, Kuca K, Jung YS.

Abstract: A series of fluorinated oxime compounds was designed and synthesized in order to probe the effect of fluorine substitution on reactivation of inhibited acetylcholinesterase (AChE) by organophosphorus agents. Permeability measurements, using the Parallel Artificial Membrane Permeation Assays (PAMPA) method, were employed to experimentally demonstrate that membrane permeabilities of the series of oximes increase in proportional to the increase in the number of fluorine atoms. Among the compounds explored in this study, the mono-fluorinated carbamoyl aldoxime 4b was the most potent reactivator for paraoxon-inhibited red blood cell (RBC) AChE.

CiteXplore: 19665386

DOI: 10.1016/j.bmc.2009.07.043