Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase
Language English Country Great Britain, England Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
16934462
DOI
10.1016/j.bmcl.2006.08.011
PII: S0960-894X(06)00900-0
Knihovny.cz E-resources
- MeSH
- Cholinesterase Inhibitors chemical synthesis chemistry pharmacology MeSH
- Nitriles chemical synthesis chemistry pharmacology MeSH
- Organophosphates pharmacology MeSH
- Paraoxon pharmacology MeSH
- Pyridinium Compounds chemical synthesis chemistry pharmacology MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- Cholinesterase Inhibitors MeSH
- Nitriles MeSH
- Organophosphates MeSH
- Paraoxon MeSH
- Pyridinium Compounds MeSH
- tabun MeSH Browser
Three asymmetrical AChE reactivators with cyano-moiety and propane linker were synthesized using modification of currently known synthetic pathways. Their potency to reactivate AChE inhibited by nerve agent tabun and insecticide paraoxon was tested in vitro and compared to pralidoxime, HI-6, obidoxime, K027, and K048. According to the results, three compounds seem to be promising against paraoxon-inhibited AChE. Better results were obtained for bisquaternary substances at least with one oxime group in position four. None of tested substances was able to satisfactorily reactivate tabun-inhibited AChE at concentration applicable for in vivo experiments.
References provided by Crossref.org
Novel Group of AChE Reactivators-Synthesis, In Vitro Reactivation and Molecular Docking Study
