Novel series of bispyridinium compounds bearing a (Z)-but-2-ene linker--synthesis and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase
Language English Country England, Great Britain Media print-electronic
Document type Journal Article, Research Support, Non-U.S. Gov't
PubMed
17383875
DOI
10.1016/j.bmcl.2007.03.025
PII: S0960-894X(07)00318-6
Knihovny.cz E-resources
- MeSH
- Acetylcholinesterase drug effects MeSH
- Butanes pharmacology MeSH
- Cholinesterase Inhibitors pharmacology MeSH
- Humans MeSH
- Organophosphates antagonists & inhibitors pharmacology MeSH
- Oximes chemical synthesis chemistry pharmacology MeSH
- Paraoxon antagonists & inhibitors pharmacology MeSH
- Pyridinium Compounds chemical synthesis chemistry pharmacology MeSH
- Cholinesterase Reactivators chemical synthesis chemistry pharmacology MeSH
- Check Tag
- Humans MeSH
- Publication type
- Journal Article MeSH
- Research Support, Non-U.S. Gov't MeSH
- Names of Substances
- 1,4-bis(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide MeSH Browser
- Acetylcholinesterase MeSH
- Butanes MeSH
- Cholinesterase Inhibitors MeSH
- K075 compound MeSH Browser
- Organophosphates MeSH
- Oximes MeSH
- Paraoxon MeSH
- Pyridinium Compounds MeSH
- Cholinesterase Reactivators MeSH
- tabun MeSH Browser
Six novel AChE reactivators with a (Z)-but-2-ene linker were synthesized using the known synthetic pathways. Their ability to reactivate AChE, which had been previously inhibited by nerve agent tabun or pesticide paraoxon, was tested in vitro and compared to pralidoxime, HI-6, obidoxime, and K075. The novel synthesized compounds were found to be ineffective against GA-inhibited AChE but the ability of (Z)-1,4-bis(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide to reactivate paraoxon-inhibited AChE was comparable with that of oxime K075. Notably, the oxime group in position four substantially increased the ability of the novel compounds to reactivate paraoxon-inhibited AChE.
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