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Statements

Subject Item
n2:RIV%2F60162694%3AG44__%2F11%3A00002456%21RIV12-MO0-G44_____
rdf:type
skos:Concept n17:Vysledek
rdfs:seeAlso
http://dx.doi.org/10.3109/14756366.2010.496362
dcterms:description
In this paper, we describe 17 novel bisquaternary compounds and analyse their effect on AChE inhibition. The newly prepared compounds were evaluated in vitro using both human erythrocyte acetylcholinesterase (AChE) and human plasmatic butyrylcholinesterase. Their inhibitory ability was expressed as an IC50 and then compared to standard carbamate drugs and two AChE reactivators. One of these novel compounds provided promising AChE inhibition (nM range) in vitro and better than the currently used standards. Additionally, a kinetics assay confirmed the non-competitive inhibition of hAChE by this novel compound. Consequently, the docking results confirmed the apparent π-π or π-cationic interactions with key amino acid residues of hAChE and the binding of the chosen compound aside enzyme catalytic site. In this paper, we describe 17 novel bisquaternary compounds and analyse their effect on AChE inhibition. The newly prepared compounds were evaluated in vitro using both human erythrocyte acetylcholinesterase (AChE) and human plasmatic butyrylcholinesterase. Their inhibitory ability was expressed as an IC50 and then compared to standard carbamate drugs and two AChE reactivators. One of these novel compounds provided promising AChE inhibition (nM range) in vitro and better than the currently used standards. Additionally, a kinetics assay confirmed the non-competitive inhibition of hAChE by this novel compound. Consequently, the docking results confirmed the apparent π-π or π-cationic interactions with key amino acid residues of hAChE and the binding of the chosen compound aside enzyme catalytic site.
dcterms:title
The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage
skos:prefLabel
The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage The preparation, in vitro screening and molecular docking of symmetrical bisquaternary cholinesterase inhibitors containing a but-(2E)-en-1,4-diyl connecting linkage
skos:notation
RIV/60162694:G44__/11:00002456!RIV12-MO0-G44_____
n5:aktivita
n12:I n12:S n12:P
n5:aktivity
I, P(OVUOFVZ200805), S
n5:cisloPeriodika
2
n5:dodaniDat
n14:2012
n5:domaciTvurceVysledku
n9:6369847 n9:9644830 n9:4641531 n9:6469922 n9:6306888 n9:3876284
n5:druhVysledku
n18:J
n5:duvernostUdaju
n11:S
n5:entitaPredkladatele
n10:predkladatel
n5:idSjednocenehoVysledku
223064
n5:idVysledku
RIV/60162694:G44__/11:00002456
n5:jazykVysledku
n19:eng
n5:klicovaSlova
cholinesterase; inhibitor; pre-treatment; Myasthenia gravis; quaternary; in vitro; docking
n5:klicoveSlovo
n6:Myasthenia%20gravis n6:docking n6:in%20vitro n6:quaternary n6:pre-treatment n6:inhibitor n6:cholinesterase
n5:kodStatuVydavatele
GB - Spojené království Velké Británie a Severního Irska
n5:kontrolniKodProRIV
[9456B44220A2]
n5:nazevZdroje
Journal of Enzyme Inhibition and Medicinal Chemistry
n5:obor
n16:FR
n5:pocetDomacichTvurcuVysledku
6
n5:pocetTvurcuVysledku
11
n5:projekt
n15:OVUOFVZ200805
n5:rokUplatneniVysledku
n14:2011
n5:svazekPeriodika
26
n5:tvurceVysledku
Musílek, Kamil Pavlíková, Růžena Doležal, Martin Gunn-Moore, Frank Holas, Ondřej Kuča, Kamil Komlóová, Markéta Marek, Jan Pohanka, Miroslav Dohnal, Vlastimil Hrabinová, Martina
n5:wos
000288441700013
s:issn
1475-6366
s:numberOfPages
9
n13:organizacniJednotka
G44