Design of a potent reactivator of tabun-inhibited acetylcholinesterase--synthesis and evaluation of (E)-1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide (K203)
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
Grantová podpora
G0400930
Medical Research Council - United Kingdom
PubMed
17924614
DOI
10.1021/jm070653r
Knihovny.cz E-zdroje
- MeSH
- acetylcholinesterasa chemie MeSH
- chemické bojové látky chemie MeSH
- cholinesterasové inhibitory chemie MeSH
- kinetika MeSH
- organofosfáty chemie MeSH
- oximy chemická syntéza chemie MeSH
- pyridinové sloučeniny chemická syntéza chemie MeSH
- racionální návrh léčiv MeSH
- reaktivátory cholinesterázy chemická syntéza chemie MeSH
- vztahy mezi strukturou a aktivitou MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1-(4-carbamoylpyridinium)-4-(4-hydroxyiminomethylpyridinium)but-2-ene MeSH Prohlížeč
- acetylcholinesterasa MeSH
- chemické bojové látky MeSH
- cholinesterasové inhibitory MeSH
- organofosfáty MeSH
- oximy MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterázy MeSH
- tabun MeSH Prohlížeč
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.
Citace poskytuje Crossref.org
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