Syntéza reaktivátorů fosforylované acetylcholinesterasy bis-pyridiniumdialdoximového typu s 3-oxapentanovým spojovacím retezcem a jejich testování in vitro na modelu enzymu inhibovaného chlorpyrifosem a methylchlorpyrifosem
[Synthesis of reactivators of phosphorylated acetylcholinesterase of bis-pyridiniumdialdoxime type with a 3-oxapentane connecting chain and their testing in vitro on a model of the enzyme inhibited by chlorpyrifos and methylchlorpyrifos]
Jazyk čeština Země Česko Médium print
Typ dokumentu anglický abstrakt, časopisecké články
PubMed
16838488
- MeSH
- acetylcholinesterasa chemie MeSH
- cholinesterasové inhibitory farmakologie MeSH
- dursban analogy a deriváty farmakologie MeSH
- fosforylace MeSH
- insekticidy farmakologie MeSH
- reaktivátory cholinesterázy chemická syntéza farmakologie MeSH
- Publikační typ
- anglický abstrakt MeSH
- časopisecké články MeSH
- Názvy látek
- acetylcholinesterasa MeSH
- cholinesterasové inhibitory MeSH
- dursban MeSH
- insekticidy MeSH
- reaktivátory cholinesterázy MeSH
Insecticides (e.g., parathion, chlorpyrifos, methylchlorpyrifos) and nerve agents (e.g.. soman, sarin, tabun, VX) belong to the group of organophosphates. They are able to irreversibly inhibit the enzyme acetylcholinesterase (AChE). Three new reactivators with a 3-oxapentane connecting chain were prepared. The ability of the new compounds to reactivate AChE inhibited by pesticides was tested in vitro and compared to known oxime 10(-3) M which is unfortunately not applicable to in vivo experiments. All tested compounds are practically ineffective for methylchlorpyrifos-inhibited AChE at the physiological concentration (10(-5) M). On the other hand, the known reactivators surpass new substances in the case of chlorpyrifos-inhibited AChE at both concentrations.
