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
Jazyk angličtina Země Anglie, Velká Británie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
17383875
DOI
10.1016/j.bmcl.2007.03.025
PII: S0960-894X(07)00318-6
Knihovny.cz E-zdroje
- MeSH
- acetylcholinesterasa účinky léků MeSH
- butany farmakologie MeSH
- cholinesterasové inhibitory farmakologie MeSH
- lidé MeSH
- organofosfáty antagonisté a inhibitory farmakologie MeSH
- oximy chemická syntéza chemie farmakologie MeSH
- paraoxon antagonisté a inhibitory farmakologie MeSH
- pyridinové sloučeniny chemická syntéza chemie farmakologie MeSH
- reaktivátory cholinesterázy chemická syntéza chemie farmakologie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- 1,4-bis(4-hydroxyiminomethylpyridinium)-but-2-ene dibromide MeSH Prohlížeč
- acetylcholinesterasa MeSH
- butany MeSH
- cholinesterasové inhibitory MeSH
- K075 compound MeSH Prohlížeč
- organofosfáty MeSH
- oximy MeSH
- paraoxon MeSH
- pyridinové sloučeniny MeSH
- reaktivátory cholinesterázy MeSH
- tabun MeSH Prohlížeč
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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