Synthesis of monooxime-monocarbamoyl bispyridinium compounds bearing (E)-but-2-ene linker and evaluation of their reactivation activity against tabun- and paraoxon-inhibited acetylcholinesterase
Language English Country Great Britain, England Media print
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
18341256
DOI
10.1080/14756360701383981
PII: 783538812
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase metabolism MeSH
- Cholinesterase Inhibitors chemistry pharmacology MeSH
- Carbamates MeSH
- Humans MeSH
- Organophosphates pharmacology MeSH
- Oximes MeSH
- Paraoxon pharmacology MeSH
- Pyridinium Compounds chemical synthesis pharmacology MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Acetylcholinesterase MeSH
- Cholinesterase Inhibitors MeSH
- Carbamates MeSH
- Organophosphates MeSH
- Oximes MeSH
- Paraoxon MeSH
- Pyridinium Compounds MeSH
- tabun MeSH Browser
Six AChE monooxime-monocarbamoyl reactivators with an (E)-but-2-ene linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by the nerve agent tabun and insecticide paraoxon was tested in vitro. The reactivation efficacies of pralidoxime, HI-6, obidoxime, K048, K075 and the newly prepared reactivators were compared. According to the results obtained, one reactivator seems to be promising against tabun-inhibited AChE and two reactivators against paraoxon-inhibited AChE. The best results were obtained for bisquaternary substances with at least one oxime group in position four.
References provided by Crossref.org
Trends in the Recent Patent Literature on Cholinesterase Reactivators (2016-2019)
