A new group of monoquaternary reactivators of acetylcholinesterase inhibited by nerve agents
Jazyk angličtina Země Velká Británie, Anglie Médium print
Typ dokumentu časopisecké články, práce podpořená grantem
- MeSH
- acetylcholinesterasa metabolismus MeSH
- kinetika MeSH
- ligandy MeSH
- molekulární struktura MeSH
- nitrofenoly metabolismus MeSH
- oximy chemická syntéza farmakologie MeSH
- pralidoximové sloučeniny chemie MeSH
- pyridinové sloučeniny chemie MeSH
- reaktivátory cholinesterázy chemická syntéza farmakologie MeSH
- synergismus léků MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 4-hydroxyiminomethyl-1-methylpyridinium iodide MeSH Prohlížeč
- 4-nitrophenyl acetate MeSH Prohlížeč
- acetylcholinesterasa MeSH
- ligandy MeSH
- nitrofenoly MeSH
- oximy MeSH
- pralidoxime MeSH Prohlížeč
- pralidoximové sloučeniny MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterázy MeSH
Reactivators of acetylcholinesterase (AChE; EC 3.1.1.7) are able to treat intoxication by organophosphorus compounds, especially with pesticides or nerve agents. Owing to the fact that there exists no universal "broad-spectrum" reactivator of organophosphates-inhibited AChE, many laboratories have synthesized new AChE reactivators. Here, we synthesized five new and three previously known quaternary monopyridinium oximes as potential reactivators of AChE inhibited by nerve agents. Potencies to cleave p-nitrophenyl acetate (PNPA), which is commonly used as a model substrate of nerve agents, were measured. Their cleaving potencies were compared with 4-PAM (4-hydroxyiminomethyl-1-methylpyridinium iodide), which is derived from the structure of the currently used AChE-reactivator 2-PAM (2-hydroxyiminomethyl-1-methylpyridinium iodide). Three newly synthesized oximes achieved similar nucleophilicity at the similar pKa according to 4-PAM, which is very promising for using these derivatives as AChE reactivators.
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