Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase
Jazyk angličtina Země Velká Británie, Anglie Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
16934462
DOI
10.1016/j.bmcl.2006.08.011
PII: S0960-894X(06)00900-0
Knihovny.cz E-zdroje
- MeSH
- cholinesterasové inhibitory chemická syntéza chemie farmakologie MeSH
- nitrily chemická syntéza chemie farmakologie MeSH
- organofosfáty farmakologie MeSH
- paraoxon farmakologie MeSH
- pyridinové sloučeniny chemická syntéza chemie farmakologie MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- cholinesterasové inhibitory MeSH
- nitrily MeSH
- organofosfáty MeSH
- paraoxon MeSH
- pyridinové sloučeniny MeSH
- tabun MeSH Prohlížeč
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.
Citace poskytuje Crossref.org
Novel Group of AChE Reactivators-Synthesis, In Vitro Reactivation and Molecular Docking Study
