Synthesis and anticholinesterase activity of new substituted benzo[d]oxazole-based derivatives
© 2016 John Wiley & Sons A/S..
A series of novel benzo[d]oxazole derivatives (6a-n) have been synthesized and biologically evaluated as potential inhibitors of acetylcholinesterases (AChE) and butyrylcholinesterase (BChE). The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro studies showed that most of the synthesized compounds are potent acetylcholinesterase and butyrylcholinesterase inhibitors. Among them, compounds 6a and 6j strongly inhibited AChE and BChE activities with IC50 values of 1.03-1.35 and 6.6-8.1 μm, respectively. Docking studies also provided the binding modes of action and identified hydrophobic pi forces as the main interaction.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2017 |
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| Erschienen: |
2017 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:89 |
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| Enthalten in: |
Chemical biology & drug design - 89(2017), 5 vom: 10. Mai, Seite 783-789 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Pouramiri, Behjat [VerfasserIn] |
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| Links: |
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| Themen: |
Acetylcholinesterase |
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| Anmerkungen: |
Date Completed 09.05.2017 Date Revised 12.10.2018 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1111/cbdd.12902 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM266340121 |
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| 520 | |a © 2016 John Wiley & Sons A/S. | ||
| 520 | |a A series of novel benzo[d]oxazole derivatives (6a-n) have been synthesized and biologically evaluated as potential inhibitors of acetylcholinesterases (AChE) and butyrylcholinesterase (BChE). The chemical structures of all final compounds were confirmed by spectroscopic methods. In vitro studies showed that most of the synthesized compounds are potent acetylcholinesterase and butyrylcholinesterase inhibitors. Among them, compounds 6a and 6j strongly inhibited AChE and BChE activities with IC50 values of 1.03-1.35 and 6.6-8.1 μm, respectively. Docking studies also provided the binding modes of action and identified hydrophobic pi forces as the main interaction | ||
| 650 | 4 | |a Journal Article | |
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| 650 | 4 | |a benzo[d]oxazol | |
| 650 | 4 | |a docking study | |
| 650 | 7 | |a Benzoxazoles |2 NLM | |
| 650 | 7 | |a Cholinesterase Inhibitors |2 NLM | |
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| 650 | 7 | |a Butyrylcholinesterase |2 NLM | |
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| 700 | 1 | |a Moghimi, Setareh |e verfasserin |4 aut | |
| 700 | 1 | |a Mahdavi, Mohammad |e verfasserin |4 aut | |
| 700 | 1 | |a Nadri, Hamid |e verfasserin |4 aut | |
| 700 | 1 | |a Moradi, Alireza |e verfasserin |4 aut | |
| 700 | 1 | |a Tavakolinejad-Kermani, Esmat |e verfasserin |4 aut | |
| 700 | 1 | |a Firoozpour, Loghman |e verfasserin |4 aut | |
| 700 | 1 | |a Asadipour, Ali |e verfasserin |4 aut | |
| 700 | 1 | |a Foroumadi, Alireza |e verfasserin |4 aut | |
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