About: Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.     Goto   Sponge   NotDistinct   Permalink

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Description
  • Bylo připraveno šest potenciálních reaktivátorů AChE a testováno na chlorpyrifosem inhibovaném enzymu. (cs)
  • 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.
  • 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. (en)
Title
  • Syntéza asymetrických bispyridiniových sloučenin s kyano skupinou a testování jejich reaktivační aktivity proti tabunem a paraoxonem inhibované acetylcholinesterase (cs)
  • Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
  • Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. (en)
skos:prefLabel
  • Syntéza asymetrických bispyridiniových sloučenin s kyano skupinou a testování jejich reaktivační aktivity proti tabunem a paraoxonem inhibované acetylcholinesterase (cs)
  • Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase.
  • Synthesis of asymmetrical bispyridinium compounds bearing cyano-moiety and evaluation of their reactivation activity against tabun and paraoxon-inhibited acetylcholinesterase. (en)
skos:notation
  • RIV/60162694:G44__/06:00001446!RIV07-MO0-G44_____
http://linked.open.../vavai/riv/strany
  • 5673-5676
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • Z(MO0FVZ0000501)
http://linked.open...iv/cisloPeriodika
  • 21
http://linked.open...vai/riv/dodaniDat
http://linked.open...aciTvurceVysledku
http://linked.open.../riv/druhVysledku
http://linked.open...iv/duvernostUdaju
http://linked.open...titaPredkladatele
http://linked.open...dnocenehoVysledku
  • 502820
http://linked.open...ai/riv/idVysledku
  • RIV/60162694:G44__/06:00001446
http://linked.open...riv/jazykVysledku
http://linked.open.../riv/klicovaSlova
  • Acetylcholinesterase; Reactivation; Nerve agent; Tabun; Pesticide; Paraoxon; Reactivator; Oxime (en)
http://linked.open.../riv/klicoveSlovo
http://linked.open...odStatuVydavatele
  • GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV
  • [7A9F2627AF1B]
http://linked.open...i/riv/nazevZdroje
  • Bioorganic and Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor
http://linked.open...ichTvurcuVysledku
http://linked.open...cetTvurcuVysledku
http://linked.open...UplatneniVysledku
http://linked.open...v/svazekPeriodika
  • 16
http://linked.open...iv/tvurceVysledku
  • Doležal, Martin
  • Dohnal, Vlastimil
  • Kuča, Kamil
  • Musílek, Kamil
  • Jun, Daniel
  • Holas, Ondřej
http://linked.open...n/vavai/riv/zamer
issn
  • 0960-894X
number of pages
http://localhost/t...ganizacniJednotka
  • G44
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