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Synthesis, in vitro acetylcholinesterase inhibitory activity and molecular docking of new acridine-coumarin hybrids
S. Hamulakova, L. Janovec, O. Soukup, D. Jun, K. Kuca,
International journal of biological macromolecules.
2017 ;
104 (Pt A) :
333-338.
[pub] 20170607
Jazyk angličtina Země Nizozemsko
Typ dokumentu časopisecké články
Perzistentní odkaz
https://www.medvik.cz/link/bmc18024955
Grantová podpora
NV15-30954A
MZ0
CEP - Centrální evidence projektů
- MeSH
- acetylcholinesterasa chemie metabolismus MeSH
- akridiny chemická syntéza chemie metabolismus farmakologie MeSH
- cholinesterasové inhibitory chemická syntéza chemie metabolismus farmakologie MeSH
- inhibiční koncentrace 50 MeSH
- katalytická doména MeSH
- kumariny chemie MeSH
- lidé MeSH
- simulace molekulového dockingu * MeSH
- techniky syntetické chemie MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
A novel series of acridine-coumarin hybrids was synthesized and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The newly synthesized derivatives 9a-d have shown higher activity against human AChE (hAChE) compared with 7-MEOTA as the standard drug. Among them derivative 9b exhibited the most potent acetylcholinesterase inhibitory activity, with an IC50 value of 5.85μM compared with 7-MEOTA (IC50=15μM). Molecular modelling studies were performed to predict the binding modes of compounds 9b, 9c and 9f with hAChE/hBuChE.
Citace poskytuje Crossref.org
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- $a Hamulakova, Slavka $u Department of Organic Chemistry, Institute of Chemical Sciences, Faculty of Science, P. J. Safarik University, Moyzesova 11, SK-041 67 Kosice, Slovak Republic. Electronic address: slavka.hamulakova@upjs.sk.
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- $a A novel series of acridine-coumarin hybrids was synthesized and biologically evaluated for their potential inhibitory effect on both acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE). The newly synthesized derivatives 9a-d have shown higher activity against human AChE (hAChE) compared with 7-MEOTA as the standard drug. Among them derivative 9b exhibited the most potent acetylcholinesterase inhibitory activity, with an IC50 value of 5.85μM compared with 7-MEOTA (IC50=15μM). Molecular modelling studies were performed to predict the binding modes of compounds 9b, 9c and 9f with hAChE/hBuChE.
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