Synthesis and Evaluation of Chroman-4-One Linked to N-Benzyl Pyridinium Derivatives as New Acetylcholinesterase Inhibitors
© 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim..
A novel series of chroman-4-one derivatives containing the N-benzyl pyridinium moiety were designed, synthesized, and evaluated for their acetylcholinesterase (AChE) inhibitory activities. Among the various synthesized compounds, (E)-1-(2,3-dibromobenzyl)-4-((7-ethoxy-4-oxochroman-3-ylidene)methyl)pyridinium bromide (8l) depicted the most potent anti-AChE activity (IC50 = 0.048 μM). In addition, the molecular modeling study allowed us to detect possible binding modes that are in full compliance with the observed results through in vitro experiments.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2015 |
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| Erschienen: |
2015 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:348 |
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| Enthalten in: |
Archiv der Pharmazie - 348(2015), 9 vom: 20. Sept., Seite 643-9 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Arab, Saman [VerfasserIn] |
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| Links: |
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| Anmerkungen: |
Date Completed 06.10.2016 Date Revised 30.12.2016 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1002/ardp.201500149 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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NLM251050661 |
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| 520 | |a © 2015 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim. | ||
| 520 | |a A novel series of chroman-4-one derivatives containing the N-benzyl pyridinium moiety were designed, synthesized, and evaluated for their acetylcholinesterase (AChE) inhibitory activities. Among the various synthesized compounds, (E)-1-(2,3-dibromobenzyl)-4-((7-ethoxy-4-oxochroman-3-ylidene)methyl)pyridinium bromide (8l) depicted the most potent anti-AChE activity (IC50 = 0.048 μM). In addition, the molecular modeling study allowed us to detect possible binding modes that are in full compliance with the observed results through in vitro experiments | ||
| 650 | 4 | |a Journal Article | |
| 650 | 4 | |a Research Support, Non-U.S. Gov't | |
| 650 | 4 | |a Acetylcholinesterase | |
| 650 | 4 | |a Alzheimer's disease | |
| 650 | 4 | |a Chroman-4-one | |
| 650 | 4 | |a Docking study | |
| 650 | 4 | |a N-Benzyl pyridinium | |
| 650 | 7 | |a Benzyl Compounds |2 NLM | |
| 650 | 7 | |a Cholinesterase Inhibitors |2 NLM | |
| 650 | 7 | |a Pyridinium Compounds |2 NLM | |
| 650 | 7 | |a Acetylcholinesterase |2 NLM | |
| 650 | 7 | |a EC 3.1.1.7 |2 NLM | |
| 700 | 1 | |a Sadat-Ebrahimi, Seyed-Esmail |e verfasserin |4 aut | |
| 700 | 1 | |a Mohammadi-Khanaposhtani, Maryam |e verfasserin |4 aut | |
| 700 | 1 | |a Moradi, Alireza |e verfasserin |4 aut | |
| 700 | 1 | |a Nadri, Hamid |e verfasserin |4 aut | |
| 700 | 1 | |a Mahdavi, Mohammad |e verfasserin |4 aut | |
| 700 | 1 | |a Moghimi, Setareh |e verfasserin |4 aut | |
| 700 | 1 | |a Asadi, Mehdi |e verfasserin |4 aut | |
| 700 | 1 | |a Firoozpour, Loghman |e verfasserin |4 aut | |
| 700 | 1 | |a Pirali-Hamedani, Morteza |e verfasserin |4 aut | |
| 700 | 1 | |a Shafiee, Abbas |e verfasserin |4 aut | |
| 700 | 1 | |a Foroumadi, Alireza |e verfasserin |4 aut | |
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