Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies
Identifikátory výsledku
Kód výsledku v IS VaVaI
<a href="https://www.isvavai.cz/riv?ss=detail&h=RIV%2F00216208%3A11110%2F13%3A10144061" target="_blank" >RIV/00216208:11110/13:10144061 - isvavai.cz</a>
Nalezeny alternativní kódy
RIV/60162694:G44__/13:43874846 RIV/00216208:11160/13:10144061 RIV/00179906:_____/13:10144061 RIV/00179906:_____/13:10218292
Výsledek na webu
<a href="http://www.ingentaconnect.com/content/ben/loc/2013/00000010/00000004/art00011" target="_blank" >http://www.ingentaconnect.com/content/ben/loc/2013/00000010/00000004/art00011</a>
DOI - Digital Object Identifier
<a href="http://dx.doi.org/10.2174/1570178611310040011" target="_blank" >10.2174/1570178611310040011</a>
Alternativní jazyky
Jazyk výsledku
angličtina
Název v původním jazyce
Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies
Popis výsledku v původním jazyce
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 withrespect 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.
Název v anglickém jazyce
Comparison of Novel Tacrine and 7-MEOTA Derivatives with Aromatic and Alicyclic Residues: Synthesis, Biological Evaluation and Docking Studies
Popis výsledku anglicky
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 withrespect 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.
Klasifikace
Druh
J<sub>x</sub> - Nezařazeno - Článek v odborném periodiku (Jimp, Jsc a Jost)
CEP obor
FR - Farmakologie a lékárnická chemie
OECD FORD obor
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Návaznosti výsledku
Projekt
<a href="/cs/project/GAP303%2F11%2F1907" target="_blank" >GAP303/11/1907: Nové inhibitory acetylcholinesterasy odvozené od látky 7-MEOTA - potenciální léčiva pro Alzheimerovu nemoc</a><br>
Návaznosti
S - Specificky vyzkum na vysokych skolach<br>I - Institucionalni podpora na dlouhodoby koncepcni rozvoj vyzkumne organizace
Ostatní
Rok uplatnění
2013
Kód důvěrnosti údajů
S - Úplné a pravdivé údaje o projektu nepodléhají ochraně podle zvláštních právních předpisů
Údaje specifické pro druh výsledku
Název periodika
Letters in Organic Chemistry
ISSN
1570-1786
e-ISSN
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Svazek periodika
10
Číslo periodika v rámci svazku
4
Stát vydavatele periodika
AE - Spojené arabské emiráty
Počet stran výsledku
7
Strana od-do
291-297
Kód UT WoS článku
000318689200010
EID výsledku v databázi Scopus
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