Abstract
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 structurally 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.
Keywords: Acetylcholinesterase, reactivators, structure-activity relationship, cyclosarin, organophosphates
Letters in Organic Chemistry
Title: Structure-Activity Relationship of Acetylcholinesterase Reactivators -Antidotes Against Nerve Agents
Volume: 4 Issue: 3
Author(s): Kamil Kuca, Veronika Racakova, Daniel Jun and Jiri Bajgar
Affiliation:
Keywords: Acetylcholinesterase, reactivators, structure-activity relationship, cyclosarin, organophosphates
Abstract: 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 structurally 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.
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Cite this article as:
Kuca Kamil, Racakova Veronika, Jun Daniel and Bajgar Jiri, Structure-Activity Relationship of Acetylcholinesterase Reactivators -Antidotes Against Nerve Agents, Letters in Organic Chemistry 2007; 4 (3) . https://dx.doi.org/10.2174/157017807780737282
DOI https://dx.doi.org/10.2174/157017807780737282 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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