Structure-activity relationship of acetylcholinesterase reactivators antidotes against nerve agents

被引：10
作者：
Kuca, Kamil
Racakova, Veronika
Jun, Daniel
Bajgar, Jiri
机构：
[1] Univ Def, Fac Mil Hlth Sci, Dept Toxicol, Hradec Kralove 50001, Czech Republic
[2] Univ Def, Ctr Adv Studies, Hradec Kralove 50001, Czech Republic
[3] Charles Univ Prague, Fac Pharm Hradec Kravloce, Dept Pharmaceut Chem & Drug Control, Hradec Kralove, Czech Republic
来源：
LETTERS IN ORGANIC CHEMISTRY | 2007年 / 4卷 / 03期
关键词：
acetylcholinesterase; reactivators; structure-activity relationship; cyclosarin; organophosphates;
D O I：
10.2174/157017807780737282
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Organophosphorus nerve agents such as sarin, cyclosarin or tabun are substances originally developed for military purposes. These compounds are able to inhibit an enzyme acetylcholinesterase (AChE; EC 3.1.1.7) via phosphorylation in its active site. AChE reactivators and anticholinergics are generally used as antidotes in the case of intoxication with these agents. In this work, reactivation potency of twenty-one struct urally different AChE reactivators was tested in vitro and subsequently, relationship between their chemical structure and biological activity was described. Cyclosarin as an appropriate member of the nerve agents family was chosen to illustrate these relationships.
引用
收藏
页码：212 / 217
页数：6
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