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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)
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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)
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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)
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skos:notation
| - RIV/00216208:11160/13:10144061!RIV14-MSM-11160___
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http://linked.open...avai/riv/aktivita
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http://linked.open...avai/riv/aktivity
| - I, O, P(GAP303/11/1907), S
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http://linked.open...iv/cisloPeriodika
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http://linked.open...vai/riv/dodaniDat
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http://linked.open...aciTvurceVysledku
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http://linked.open.../riv/druhVysledku
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http://linked.open...iv/duvernostUdaju
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http://linked.open...titaPredkladatele
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http://linked.open...dnocenehoVysledku
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http://linked.open...ai/riv/idVysledku
| - RIV/00216208:11160/13:10144061
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http://linked.open...riv/jazykVysledku
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http://linked.open.../riv/klicovaSlova
| - molecular modelling; inhibition selectivity; butyrylcholinesterase; Alzheimer's disease; acetylcholinesterase; 7-methoxytacrine (en)
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http://linked.open.../riv/klicoveSlovo
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http://linked.open...odStatuVydavatele
| - AE - Stát Spojené arabské emiráty
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http://linked.open...ontrolniKodProRIV
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http://linked.open...i/riv/nazevZdroje
| - Letters in Organic Chemistry
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http://linked.open...in/vavai/riv/obor
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http://linked.open...ichTvurcuVysledku
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http://linked.open...cetTvurcuVysledku
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http://linked.open...vavai/riv/projekt
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http://linked.open...UplatneniVysledku
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http://linked.open...v/svazekPeriodika
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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
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http://linked.open...ain/vavai/riv/wos
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issn
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number of pages
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http://bibframe.org/vocab/doi
| - 10.2174/1570178611310040011
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http://localhost/t...ganizacniJednotka
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