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]
Language Czech Country Czech Republic Media print
Document type English Abstract, Journal Article
PubMed
16838488
- MeSH
- Acetylcholinesterase chemistry MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Chlorpyrifos analogs & derivatives pharmacology MeSH
- Phosphorylation MeSH
- Insecticides pharmacology MeSH
- Cholinesterase Reactivators chemical synthesis pharmacology MeSH
- Publication type
- English Abstract MeSH
- Journal Article MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Cholinesterase Inhibitors MeSH
- Chlorpyrifos MeSH
- Insecticides MeSH
- Cholinesterase Reactivators 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.
