About: 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     Goto   Sponge   NotDistinct   Permalink

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  • 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 paraoxoninhibited 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.
  • 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 paraoxoninhibited 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. (en)
  • Byla připravena série nových reaktivátorů acetylcholinesterasy s (Z)-but-2-enovým spojovacím řetězcem - Syntéza a jejich testování proti tabunem a paraoxonem inhibované acetylcholinesterase. (cs)
Title
  • 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
  • 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 (en)
  • Série nových reaktivátorů acetylcholinesterasy s (Z)-but-2-enovým spojovacím řetězcem - Syntéza a jejich testování proti tabunem a paraoxonem inhibované acetylcholinesterase (cs)
skos:prefLabel
  • 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
  • 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 (en)
  • Série nových reaktivátorů acetylcholinesterasy s (Z)-but-2-enovým spojovacím řetězcem - Syntéza a jejich testování proti tabunem a paraoxonem inhibované acetylcholinesterase (cs)
skos:notation
  • RIV/60162694:G44__/07:00001766!RIV08-MO0-G44_____
http://linked.open.../vavai/riv/strany
  • 3172-3176
http://linked.open...avai/riv/aktivita
http://linked.open...avai/riv/aktivity
  • V, Z(MO0FVZ0000501)
http://linked.open...iv/cisloPeriodika
  • 11
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
  • 437922
http://linked.open...ai/riv/idVysledku
  • RIV/60162694:G44__/07:00001766
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
  • [3C5CB2804894]
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
  • 17
http://linked.open...iv/tvurceVysledku
  • Doležal, Martin
  • Dohnal, Vlastimil
  • Kuča, Kamil
  • Musílek, Kamil
  • Jun, Daniel
  • Opletalová, Veronika
  • Holas, Ondřej
http://linked.open...n/vavai/riv/zamer
issn
  • 0960-894X
number of pages
http://localhost/t...ganizacniJednotka
  • G44
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