About: Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies

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An Entity of Type : http://linked.opendata.cz/ontology/domain/vavai/Vysledek, within Data Space : linked.opendata.cz associated with source document(s)

Attributes	Values
rdf:type	skos:Concept http://linked.opendata.cz/ontology/domain/vavai/Vysledek
rdfs:seeAlso	http://www.ingentaconnect.com/content/ben/loc/2013/00000010/00000004/art00011
Description	Cholinesterase inhibitors play an essential role in the treatment of Alzheimer's disease. Since their first introduction over a decade ago, they are an indispensable part of Alzheimer's disease therapy and remain at the forefront of scientific interest worldwide. In this manuscript new analogs of THA and 7-MEOTA were designed, synthesized, and evaluated for their inhibitory activity against both acetylcholinesterase and butyrylcholinesterase. Cholinergic properties were investigated and quantified with respect to their side chain residues (aromatic or alicyclic). All synthesized compounds proved to have potent inhibitory activity at micromolar range. Moreover, compound 4 demonstrated promising efficacy and appears to be an ideal candidate for further testing. Cholinesterase inhibitors play an essential role in the treatment of Alzheimer's disease. Since their first introduction over a decade ago, they are an indispensable part of Alzheimer's disease therapy and remain at the forefront of scientific interest worldwide. In this manuscript new analogs of THA and 7-MEOTA were designed, synthesized, and evaluated for their inhibitory activity against both acetylcholinesterase and butyrylcholinesterase. Cholinergic properties were investigated and quantified with respect to their side chain residues (aromatic or alicyclic). All synthesized compounds proved to have potent inhibitory activity at micromolar range. Moreover, compound 4 demonstrated promising efficacy and appears to be an ideal candidate for further testing. (en)
Title	Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies (en)
skos:prefLabel	Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies (en)
skos:notation	RIV/00216208:11160/13:10144061!RIV14-MSM-11160___
http://linked.open...avai/riv/aktivita	I O P S
http://linked.open...avai/riv/aktivity	I, O, P(GAP303/11/1907), S
http://linked.open...iv/cisloPeriodika	4
http://linked.open...vai/riv/dodaniDat	2014
http://linked.open...aciTvurceVysledku	Nepovimová, Eugenie Opletalová, Veronika
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	Univerzita Karlova v Praze / Farmaceutická fakulta v Hradci Králové
http://linked.open...dnocenehoVysledku	66267
http://linked.open...ai/riv/idVysledku	RIV/00216208:11160/13:10144061
http://linked.open...riv/jazykVysledku	eng - angličtina
http://linked.open.../riv/klicovaSlova	molecular modelling; inhibition selectivity; butyrylcholinesterase; Alzheimer's disease; acetylcholinesterase; 7-methoxytacrine (en)
http://linked.open.../riv/klicoveSlovo	7-methoxytacrine inhibition selectivity Alzheimer's disease acetylcholinesterase butyrylcholinesterase molecular modelling
http://linked.open...odStatuVydavatele	AE - Stát Spojené arabské emiráty
http://linked.open...ontrolniKodProRIV	[1FF24F86A4EA]
http://linked.open...i/riv/nazevZdroje	Letters in Organic Chemistry
http://linked.open...in/vavai/riv/obor	FR
http://linked.open...ichTvurcuVysledku	2 (xsd:int)
http://linked.open...cetTvurcuVysledku	12 (xsd:int)
http://linked.open...vavai/riv/projekt	Novel inhibitors of acetylcholinesterase derived from 7-MEOTA - potential Alzheimer´s disease drugs
http://linked.open...UplatneniVysledku	2013
http://linked.open...v/svazekPeriodika	10
http://linked.open...iv/tvurceVysledku	Doležal, Rafael Fišar, Zdeněk Hroudová, Jana Jung, Young-Sik Kuča, Kamil Musílek, Kamil Zemek, Filip Korábečný, Jan Opletalová, Veronika Janovec, Ladislav Horová, Anna Nepovimová, Eugenie
http://linked.open...ain/vavai/riv/wos	000318689200010
issn	1570-1786
number of pages	7 (xsd:int)
http://bibframe.org/vocab/doi	10.2174/1570178611310040011
http://localhost/t...ganizacniJednotka	11160

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