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Statements

Subject Item
n2:RIV%2F67985858%3A_____%2F10%3A00342827%21RIV11-AV0-67985858
rdf:type
skos:Concept n15:Vysledek
dcterms:description
New cholinesterase reactivators are synthesized as potential antidotes for treatment of organophosphorus agent poisonings or as part of pseudo catalytic scavengers for improvement of the nerve agent prophylaxis. In this study, three novel potential cholinesterase reactivators (K064 - (E)-1-(pyridinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K065 - (E)-1-(quinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K066 - (E)-1-(isoquinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide) were synthesized and tested for their potency to reactivate acetylcholinesterase (AChE, EC 3.1.1.3) and butyrylcholinesterase (BChE, 3.1.1.8) inhibited by pesticide paraoxon. As resulted, none from the synthesized compounds surpassed currently clinically used reactivators (pralidoxime, obidoxime and HI-6). New cholinesterase reactivators are synthesized as potential antidotes for treatment of organophosphorus agent poisonings or as part of pseudo catalytic scavengers for improvement of the nerve agent prophylaxis. In this study, three novel potential cholinesterase reactivators (K064 - (E)-1-(pyridinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K065 - (E)-1-(quinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide; K066 - (E)-1-(isoquinolinium)-4-(2-hydroxyiminomethylpyridinium)-but-2-ene dibromide) were synthesized and tested for their potency to reactivate acetylcholinesterase (AChE, EC 3.1.1.3) and butyrylcholinesterase (BChE, 3.1.1.8) inhibited by pesticide paraoxon. As resulted, none from the synthesized compounds surpassed currently clinically used reactivators (pralidoxime, obidoxime and HI-6).
dcterms:title
Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases
skos:prefLabel
Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases Novel Nucleophilic Compounds with Oxime Group as Reactivators of Paraoxon-Inhibited Cholinesterases
skos:notation
RIV/67985858:_____/10:00342827!RIV11-AV0-67985858
n3:aktivita
n16:Z n16:I n16:P
n3:aktivity
I, P(IAA603020901), P(OVUOFVZ200902), Z(AV0Z40720504)
n3:cisloPeriodika
4
n3:dodaniDat
n7:2011
n3:domaciTvurceVysledku
n8:4633024
n3:druhVysledku
n18:J
n3:duvernostUdaju
n14:S
n3:entitaPredkladatele
n17:predkladatel
n3:idSjednocenehoVysledku
275445
n3:idVysledku
RIV/67985858:_____/10:00342827
n3:jazykVysledku
n9:eng
n3:klicovaSlova
acetylcholinesterase; butyrylcholinesterase; nerve agent
n3:klicoveSlovo
n6:acetylcholinesterase n6:butyrylcholinesterase n6:nerve%20agent
n3:kodStatuVydavatele
US - Spojené státy americké
n3:kontrolniKodProRIV
[853B685EE438]
n3:nazevZdroje
Letters in Drug Design & Discovery
n3:obor
n4:CC
n3:pocetDomacichTvurcuVysledku
1
n3:pocetTvurcuVysledku
9
n3:projekt
n5:OVUOFVZ200902 n5:IAA603020901
n3:rokUplatneniVysledku
n7:2010
n3:svazekPeriodika
7
n3:tvurceVysledku
Hrabinová, M. Pohanka, M. Církva, Vladimír Paleček, J. Musilová, L. Kuca, K. Paar, M. Musílek, K. Jun, D.
n3:wos
000275929300006
n3:zamer
n13:AV0Z40720504
s:issn
1570-1808
s:numberOfPages
5