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Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase
Musilek K, Holas O, Kuca K, Jun D, Dohnal V, Dolezal M.
Jazyk angličtina Země Velká Británie
NLK
ScienceDirect (archiv)
od 1993-01-01 do 2009-12-31
- MeSH
- cholinesterasové inhibitory farmakologie chemická syntéza chemie MeSH
- financování organizované MeSH
- nitrily farmakologie chemická syntéza chemie MeSH
- organofosfáty farmakologie MeSH
- paraoxon farmakologie MeSH
- pyridinové sloučeniny farmakologie chemická syntéza chemie MeSH
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.
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- $a Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase / $c Musilek K, Holas O, Kuca K, Jun D, Dohnal V, Dolezal M.
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- $a Department of Pharmaceutical Chemistry and Drug Control, Faculty of Pharmacy in Hradec Kralove, Charles University in Prague, Heyrovskeho 1203, 50005 Hradec Kralove, Czech Republic
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- $a 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.
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