About: Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage - initial study for Myasthenia gravis implications

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About: Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage - initial study for Myasthenia gravis implications Goto Sponge NotDistinct Permalink

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Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.sciencedirect.com/science/article/pii/S0960894X10000466
Description	This paper describes 20 newly prepared bispyridinium inhibitors of potential concern for Myasthenia gravis (MG). The newly prepared compounds were evaluated in vitro on human erythrocyte acetylcholinesterase (AChE) and human plasmatic butyrylcholinesterase (BChE). Their inhibitory ability was expressed as IC50 and compared to standard carbamate drugs. Three compounds presented promising inhibition (in µM range) of both enzymes in vitro similar to the used standards. The novel inhibitors did not present selectivity between AChE and BChE. Two newly prepared compounds were chosen for docking studies and confirmed apparent pí-pí or pí-cationic interactions aside enzyme's catalytic sites. The kinetics assay confirmed non-competitive inhibition of AChE by two best newly prepared compounds. This paper describes 20 newly prepared bispyridinium inhibitors of potential concern for Myasthenia gravis (MG). The newly prepared compounds were evaluated in vitro on human erythrocyte acetylcholinesterase (AChE) and human plasmatic butyrylcholinesterase (BChE). Their inhibitory ability was expressed as IC50 and compared to standard carbamate drugs. Three compounds presented promising inhibition (in µM range) of both enzymes in vitro similar to the used standards. The novel inhibitors did not present selectivity between AChE and BChE. Two newly prepared compounds were chosen for docking studies and confirmed apparent pí-pí or pí-cationic interactions aside enzyme's catalytic sites. The kinetics assay confirmed non-competitive inhibition of AChE by two best newly prepared compounds. (en)
Title	Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage - initial study for Myasthenia gravis implications Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage - initial study for Myasthenia gravis implications (en)
skos:prefLabel	Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage - initial study for Myasthenia gravis implications Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage - initial study for Myasthenia gravis implications (en)
skos:notation	RIV/60162694:G44__/10:00002231!RIV13-GA0-G44_____
http://linked.open...avai/riv/aktivita	I P S
http://linked.open...avai/riv/aktivity	I, P(GP203/09/P130), P(OVUOFVZ200805), S
http://linked.open...iv/cisloPeriodika	5
http://linked.open...vai/riv/dodaniDat	2013
http://linked.open...aciTvurceVysledku	Hrabinová, Martina Kuča, Kamil Musílek, Kamil Pohanka, Doc. RNDr. PhD, Miroslav
http://linked.open.../riv/druhVysledku	J - Článek v odborném periodiku
http://linked.open...iv/duvernostUdaju	S - Úplné a pravdivé údaje nepodléhající ochraně podle zvláštních právních předpisů
http://linked.open...titaPredkladatele	Ministerstvo obrany / Univerzita obrany - Fakulta vojenského zdravotnictví Hradec Králové
http://linked.open...dnocenehoVysledku	223066
http://linked.open...ai/riv/idVysledku	RIV/60162694:G44__/10:00002231
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	docking; in vitro; quaternary; Myasthenia gravis; inhibitor; cholinesterase (en)
http://linked.open.../riv/klicoveSlovo	cholinesterase docking quaternary in vitro Myasthenia gravis inhibitor
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[6E7CF2E98538]
http://linked.open...i/riv/nazevZdroje	Bioorganic & Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	4 (xsd:int)
http://linked.open...cetTvurcuVysledku	11 (xsd:int)
http://linked.open...vavai/riv/projekt	Development of novel acetylcholinesterase inhibitors as treatment of Myasthenia Gravis Novel inhibitors of acetylcholinesterase as prophylaxis of nerve agent poisonings
http://linked.open...UplatneniVysledku	2010
http://linked.open...v/svazekPeriodika	20
http://linked.open...iv/tvurceVysledku	Doležal, Martin Dohnal, Vlastimil Hrabinová, Martina Jung, Young-Sik Kuča, Kamil Musílek, Kamil Pohanka, Miroslav Holas, Ondřej Komlóová, Markéta Nachon, Florian Závadová, Vlasta
http://linked.open...ain/vavai/riv/wos	000274714600067
issn	0960-894X
number of pages	4 (xsd:int)
http://bibframe.org/vocab/doi	10.1016/j.bmcl.2010.01.034
http://localhost/t...ganizacniJednotka	G44

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