Structure-Activity Relationship for the Reactivators of Acetylcholinesterase Inhibited by Nerve Agent VX

Author(s): Kamil Kuca, Kamil Musilek, Daniel Jun, Jana Karasova, Ondrej Soukup, Jaroslav Pejchal, Martina Hrabinova.

Journal Name: Medicinal Chemistry

Volume 9 , Issue 5 , 2013

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Abstract:

Nerve agents such as sarin, VX and tabun are organophosphorus compounds able to inhibit an enzyme acetylcholinesterase (AChE). AChE reactivators and anticholinergics are generally used as antidotes in the case of intoxication with these agents. None from the known AChE reactivators is able to reactivate AChE inhibited by all kinds of nerve agents. In this work, reactivation potency of seventeen structurally different AChE reactivators was tested in vitro and subsequently, relationship between their chemical structure and biological activity was outlined. VX was chosen as appropriate member of the nerve agent family.

Keywords: Nerve agent, VX, Reactivation, Acetylcholinesterase, Oxime.

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Article Details

VOLUME: 9
ISSUE: 5
Year: 2013
Page: [689 - 693]
Pages: 5
DOI: 10.2174/1573406411309050008
Price: $58

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