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

被引：30

作者：

Jeong, Hee Chun ^{[3
]}

Park, No-Joong ^{[3
]}

Chae, Chong Hak ^{[3
]}

Musilek, Kamil ^{[1
]}

Kassa, Jiri ^{[1
]}

Kuca, Kamil ^{[1
,2
]}

Jung, Young-Sik ^{[3
]}

机构：

[1] Fac Mil Hlth Sci, Dept Toxicol, Hradec Kralove, Czech Republic

[2] Fac Mil Hlth Sci, Ctr Adv Studies, Hradec Kralove, Czech Republic

[3] Korea Res Inst Chem Technol, Bioorgan Sci Div, Taejon 305600, South Korea

来源：

BIOORGANIC & MEDICINAL CHEMISTRY | 2009年 / 17卷 / 17期

关键词：

Organophosphorus agents; Acetylcholinesterase; Fluorinated pyridinium oxime; Oxime reactivators; DESIGN;

D O I：

10.1016/j.bmc.2009.07.043

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

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. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：6213 / 6217

页数：5

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