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Structure—activity relationships for in vitro oxime reactivation of chlorpyrifos-inhibited acetylcholinesterase

  • K. Kuča EMAIL logo , V. Račáková and D. Jun
Published/Copyright: August 1, 2007
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Abstract

Organophosphorus pesticides parathion, chlorpyrifos, and malathion inhibit the enzyme acetylcholinesterase (AChE; EC 3.1.1.7) via phosphorylation of its active site. AChE reactivators and anticholinergics are compounds used as antidotes in the case of intoxication by these AChE inhibitors. In this work, chlorpyrifos, a representative member of this pesticide family, was used to inhibit the AChE activity of rat brain. The effect of twenty-one structurally different AChE reactivators was tested in vitro and subsequently, the relationship between their chemical structure and biological activity was outlined.

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Published Online: 2007-8-1
Published in Print: 2007-8-1

© 2007 Institute of Chemistry, Slovak Academy of Sciences

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