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Statements

Subject Item
n2:RIV%2F60162694%3AG44__%2F08%3A00002002%21RIV09-MSM-G44_____
rdf:type
skos:Concept n12:Vysledek
dcterms:description
Bylo připraveno osmnáct monokvarterních sloučenin s modifikovaných bočním řetězcem, které byly testovány proti tabunem a paraoxonem inhibované acetylcholinesterase. Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Eighteen monoquaternary reactivators of acetylcholinesterase with modified side chain were developed in an effort to extend the properties of pralidoxime. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) and the prepared compounds were tested in vitro on a model of tabun and paraoxon-inhibited AChE. Monoquaternary reactivators were not able to exceed the best known compounds for tabun poisoning, but some of them did show reactivation better or comparable with pralidoxime for paraoxon poisoning. However, extensive differences were found by a SAR study for various side chains on the non-oxime part of the reactivator molecule. Acetylcholinesterase reactivators are crucial antidotes for the treatment of organophosphate intoxication. Eighteen monoquaternary reactivators of acetylcholinesterase with modified side chain were developed in an effort to extend the properties of pralidoxime. The known reactivators (pralidoxime, HI-6, obidoxime, trimedoxime, methoxime) and the prepared compounds were tested in vitro on a model of tabun and paraoxon-inhibited AChE. Monoquaternary reactivators were not able to exceed the best known compounds for tabun poisoning, but some of them did show reactivation better or comparable with pralidoxime for paraoxon poisoning. However, extensive differences were found by a SAR study for various side chains on the non-oxime part of the reactivator molecule.
dcterms:title
Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase Monokvarterní pyridiniové soli s modifikovaných bočním řetězcem - syntéza a evaluace na modelu acetylcholinesterasy inhibované tabunem a paraoxonem Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase
skos:prefLabel
Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase Monokvarterní pyridiniové soli s modifikovaných bočním řetězcem - syntéza a evaluace na modelu acetylcholinesterasy inhibované tabunem a paraoxonem Monoquaternary pyridinium salts with modified side chain - synthesis and evaluation on model of tabun- and paraoxon-inhibited acetylcholinesterase
skos:notation
RIV/60162694:G44__/08:00002002!RIV09-MSM-G44_____
n3:aktivita
n15:S n15:P
n3:aktivity
P(ME 865), S
n3:cisloPeriodika
17
n3:dodaniDat
n14:2009
n3:domaciTvurceVysledku
n4:6306888 n4:6469922 n4:4185137
n3:druhVysledku
n13:J
n3:duvernostUdaju
n11:S
n3:entitaPredkladatele
n18:predkladatel
n3:idSjednocenehoVysledku
380556
n3:idVysledku
RIV/60162694:G44__/08:00002002
n3:jazykVysledku
n17:eng
n3:klicovaSlova
acetylcholinesterase; tabun; paraoxon; reactivator; oxime; monoquaternary
n3:klicoveSlovo
n6:acetylcholinesterase n6:monoquaternary n6:tabun n6:paraoxon n6:oxime n6:reactivator
n3:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n3:kontrolniKodProRIV
[CC5AB7A1B941]
n3:nazevZdroje
Bioorganic & Medicinal Chemistry
n3:obor
n16:FP
n3:pocetDomacichTvurcuVysledku
3
n3:pocetTvurcuVysledku
6
n3:projekt
n8:ME%20865
n3:rokUplatneniVysledku
n14:2008
n3:svazekPeriodika
16
n3:tvurceVysledku
Dohnal, Vlastimil Opletalová, Veronika Kuča, Kamil Kučera, Jiří Musílek, Kamil Jun, Daniel
n3:wos
000258827800041
s:issn
0968-0896
s:numberOfPages
6
n9:organizacniJednotka
G44