Synthesis of the novel series of bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against chlorpyrifos-inhibited acetylcholinesterase
Language English Country England, Great Britain Media print-electronic
Document type Evaluation Study, Journal Article, Research Support, Non-U.S. Gov't
PubMed
16288867
DOI
10.1016/j.bmcl.2005.10.059
PII: S0960-894X(05)01322-3
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase metabolism MeSH
- Hydrocarbons, Brominated chemical synthesis pharmacology MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Chlorpyrifos pharmacology MeSH
- Nitrogen chemistry MeSH
- Rats MeSH
- Oximes chemistry MeSH
- Pyridinium Compounds chemical synthesis pharmacology MeSH
- Cholinesterase Reactivators pharmacology MeSH
- Dose-Response Relationship, Drug MeSH
- Animals MeSH
- Check Tag
- Rats MeSH
- Animals MeSH
- Publication type
- Journal Article MeSH
- Evaluation Study MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- (E)-1-(2-hydroxyiminomethylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide MeSH Browser
- Acetylcholinesterase MeSH
- Hydrocarbons, Brominated MeSH
- Cholinesterase Inhibitors MeSH
- Chlorpyrifos MeSH
- Nitrogen MeSH
- Oximes MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators MeSH
Six potential AChE reactivators were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by insecticide chlorpyrifos was tested in vitro. According to the results, (E)-1-(2-hydroxyiminomethylpyridinium)-4-(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide seems to be the most potent AChE reactivator. The reactivation potency of these compounds depends on structural factors such as constitution of the linking chain between both pyridinium rings, position of the oxime moiety at the pyridinium ring and presence of quaternary nitrogens.
References provided by Crossref.org
Two step synthesis of a non-symmetric acetylcholinesterase reactivator
