Design of a Potent Reactivator of Tabun-Inhibited AcetylcholinesteraseSynthesis and
Evaluation of (E)-1-(4-Carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene
Dibromide (K203)
Posted on 2007-11-01 - 00:00
Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication.
Among the organophosphates, with the exception of soman, tabun (GA) intoxications are the least responsive
to treatment with commercially available therapeutics. A rational design was used to increase reactivation
ability and decrease the toxicity of the novel reactivator. (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203) has better properties than previously tested compounds
in vitro and, therefore, is a potential candidate for the treatment of GA intoxication in vivo.
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Musilek, Kamil; Jun, Daniel; Cabal, Jiri; Kassa, Jiri; Gunn-Moore, Frank; Kuca, Kamil (2016). Design of a Potent Reactivator of Tabun-Inhibited AcetylcholinesteraseSynthesis and
Evaluation of (E)-1-(4-Carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene
Dibromide (K203). ACS Publications. Collection. https://doi.org/10.1021/jm070653r
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AUTHORS (6)
KM
Kamil Musilek
DJ
Daniel Jun
JC
Jiri Cabal
JK
Jiri Kassa
FG
Frank Gunn-Moore
KK
Kamil Kuca