Design, synthesis and evaluation of aminothiazole derivatives as potential anti-Alzheimer's candidates
Aim: The objective of the present study was to design, synthesize and evaluate diverse Schiff bases and thiazolidin-4-one derivatives of aminothiazole as key pharmacophores possessing acetylcholinesterase inhibitory activity. Materials & methods: Two series of compounds (13 each) were synthesized and evaluated for their acetylcholinesterase inhibition and antioxidant activity. Molecular docking of all compounds was performed to provide an insight into their binding interactions. Results: Compounds 2j (IC50 = 0.03 μM) and 3e (IC50 = 1.58 μM) were found to be the best acetylcholinesterase inhibitors among compounds of their respective series. Molecular docking analysis supported the results of in vitro activity by displaying good docking scores with the binding pocket of human acetylcholinesterase (Protein Data Bank ID: 4EY7). Conclusion: Compound 2j emerged as a potential lead compound with excellent acetylcholinesterase inhibition, antioxidant and chelation activity.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2024 |
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| Erschienen: |
2024 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:16 |
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| Enthalten in: |
Future medicinal chemistry - 16(2024), 6 vom: 20. Feb., Seite 513-529 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Soni, Arti [VerfasserIn] |
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| Links: |
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| Themen: |
2-aminothiazole |
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| Anmerkungen: |
Date Completed 27.02.2024 Date Revised 27.02.2024 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.4155/fmc-2023-0290 |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM368656500 |
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| 520 | |a Aim: The objective of the present study was to design, synthesize and evaluate diverse Schiff bases and thiazolidin-4-one derivatives of aminothiazole as key pharmacophores possessing acetylcholinesterase inhibitory activity. Materials & methods: Two series of compounds (13 each) were synthesized and evaluated for their acetylcholinesterase inhibition and antioxidant activity. Molecular docking of all compounds was performed to provide an insight into their binding interactions. Results: Compounds 2j (IC50 = 0.03 μM) and 3e (IC50 = 1.58 μM) were found to be the best acetylcholinesterase inhibitors among compounds of their respective series. Molecular docking analysis supported the results of in vitro activity by displaying good docking scores with the binding pocket of human acetylcholinesterase (Protein Data Bank ID: 4EY7). Conclusion: Compound 2j emerged as a potential lead compound with excellent acetylcholinesterase inhibition, antioxidant and chelation activity | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Kumar, Vivek |e verfasserin |4 aut | |
| 700 | 1 | |a Rawat, Ravi |e verfasserin |4 aut | |
| 700 | 1 | |a Eyupoglu, Volkan |e verfasserin |4 aut | |
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