About: Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease

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About: Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease Goto Sponge Distinct Permalink

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rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
Description	In this paper, series of 7-MEOTA analogues (N-alkyl-7-methoxytacrine) were synthesized. Their inhibitory ability was evaluated on recombinant human acetylcholinesterase (AChE) and plasmatic human butyrylcholinesterase (BChE). Three novel compounds showed promising results towards hAChE better to THA or 7-MEOTA. Three compounds resulted as potent inhibitors of hBChE. The SAR findings highlighted the C6-C7 N-alkyl chains for cholinesterase inhibition. In this paper, series of 7-MEOTA analogues (N-alkyl-7-methoxytacrine) were synthesized. Their inhibitory ability was evaluated on recombinant human acetylcholinesterase (AChE) and plasmatic human butyrylcholinesterase (BChE). Three novel compounds showed promising results towards hAChE better to THA or 7-MEOTA. Three compounds resulted as potent inhibitors of hBChE. The SAR findings highlighted the C6-C7 N-alkyl chains for cholinesterase inhibition. (en)
Title	Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease (en)
skos:prefLabel	Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease (en)
skos:notation	RIV/60162694:G44__/10:00002299!RIV11-MO0-G44_____
http://linked.open...avai/riv/aktivita	P S
http://linked.open...avai/riv/aktivity	P(OVUOFVZ200805), S
http://linked.open...iv/cisloPeriodika	20
http://linked.open...vai/riv/dodaniDat	2011
http://linked.open...aciTvurceVysledku	Zemek, Filip Kuča, Kamil Musílek, Kamil Pohanka, Doc. RNDr. PhD, Miroslav Marek, Jan
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	291482
http://linked.open...ai/riv/idVysledku	RIV/60162694:G44__/10:00002299
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	acetylcholinesterase; butyrylcholinesterase; Alzheimer disease; tacrine; 7-MEOTA; inhibition (en)
http://linked.open.../riv/klicoveSlovo	7-MEOTA tacrine inhibition Alzheimer disease acetylcholinesterase butyrylcholinesterase
http://linked.open...odStatuVydavatele	GB - Spojené království Velké Británie a Severního Irska
http://linked.open...ontrolniKodProRIV	[8D32DCD8C62F]
http://linked.open...i/riv/nazevZdroje	Bioorganic & Medicinal Chemistry Letters
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	5 (xsd:int)
http://linked.open...cetTvurcuVysledku	10 (xsd:int)
http://linked.open...vavai/riv/projekt	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	Dohnal, Vlastimil Kuča, Kamil Marek, Jan Musílek, Kamil Pohanka, Miroslav Zemek, Filip Korábečný, Jan Opletalová, Veronika Holas, Ondřej Binder, Jiří
http://linked.open...ain/vavai/riv/wos	000281963700030
issn	0960-894X
number of pages	3 (xsd:int)
http://localhost/t...ganizacniJednotka	G44

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