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Statements

Subject Item
n2:RIV%2F60162694%3AG44__%2F13%3A43874790%21RIV14-MZ0-G44_____
rdf:type
skos:Concept n17:Vysledek
rdfs:seeAlso
http://www.stmconnect.com/sites/default/files/41-43%20%20JEIT-D-12-00014.pdf
dcterms:description
Cholinesterase reactivators are a group of drugs originally developed as antidotes for treatment of nerve agent intoxications. Although there are five commercially available members of this group, none is considered to be a universal solution for treatment of intoxication caused by all nerve agents. Due to this, novel drug candidates are searched. To find the most promising antidotes, structure activity studies are conducted. In this contribution, distance between quaternary nitrogen and aldoxime (called oxime) group responsible for the reactivation process is discussed. For this purpose, three structurally different oxime reactivators were tested for their potency to reactivate tabun, sarin, cyclosarin and VX agent-inhibited acetylcholinesterase (AC hE; EC 3.1.1.7). As resulted, only %22standard%22 oxime reactivators with oxime group connected to the heteroaromatic ring could be considered as promising AC hE reactivators. Those with oxime group on other aromatic ring or those with quaternary nitrogen excluded from heteroarenium ring did not display any reactivation. Cholinesterase reactivators are a group of drugs originally developed as antidotes for treatment of nerve agent intoxications. Although there are five commercially available members of this group, none is considered to be a universal solution for treatment of intoxication caused by all nerve agents. Due to this, novel drug candidates are searched. To find the most promising antidotes, structure activity studies are conducted. In this contribution, distance between quaternary nitrogen and aldoxime (called oxime) group responsible for the reactivation process is discussed. For this purpose, three structurally different oxime reactivators were tested for their potency to reactivate tabun, sarin, cyclosarin and VX agent-inhibited acetylcholinesterase (AC hE; EC 3.1.1.7). As resulted, only %22standard%22 oxime reactivators with oxime group connected to the heteroaromatic ring could be considered as promising AC hE reactivators. Those with oxime group on other aromatic ring or those with quaternary nitrogen excluded from heteroarenium ring did not display any reactivation.
dcterms:title
Influence of the distance between quaternary nitrogen and oxime group on the reactivation ability of oximes - antidotes against nerve agents Influence of the distance between quaternary nitrogen and oxime group on the reactivation ability of oximes - antidotes against nerve agents
skos:prefLabel
Influence of the distance between quaternary nitrogen and oxime group on the reactivation ability of oximes - antidotes against nerve agents Influence of the distance between quaternary nitrogen and oxime group on the reactivation ability of oximes - antidotes against nerve agents
skos:notation
RIV/60162694:G44__/13:43874790!RIV14-MZ0-G44_____
n4:aktivita
n13:P
n4:aktivity
P(NT12062)
n4:cisloPeriodika
1
n4:dodaniDat
n16:2014
n4:domaciTvurceVysledku
n9:6306888 n9:4898737 n9:8866651 n9:4185137 n9:4592174 n9:4641531
n4:druhVysledku
n10:J
n4:duvernostUdaju
n18:S
n4:entitaPredkladatele
n20:predkladatel
n4:idSjednocenehoVysledku
79984
n4:idVysledku
RIV/60162694:G44__/13:43874790
n4:jazykVysledku
n6:eng
n4:klicovaSlova
acetylcholinesterase; antidote; nerve agent; reactivator; oxime
n4:klicoveSlovo
n5:antidote n5:reactivator n5:nerve%20agent n5:oxime n5:acetylcholinesterase
n4:kodStatuVydavatele
US - Spojené státy americké
n4:kontrolniKodProRIV
[5B7733A9E207]
n4:nazevZdroje
Journal of Environmental Immunology and Toxicology
n4:obor
n12:FR
n4:pocetDomacichTvurcuVysledku
6
n4:pocetTvurcuVysledku
7
n4:projekt
n14:NT12062
n4:rokUplatneniVysledku
n16:2013
n4:svazekPeriodika
1
n4:tvurceVysledku
Musílek, Kamil Hrabinová, Martina Žďárová Karasová, Jana Jun, Daniel Soukup, Ondřej Korábečný, Jan Kuča, Kamil
s:issn
2225-1219
s:numberOfPages
3
n11:doi
10.7178/jeit.16
n3:organizacniJednotka
G44