Synthesis of novel thiazole derivatives against Alzheimer’s disease and investigation of their cholinesterase inhibition and antioxidant properties
Year 2024,
Volume: 3 Issue: 3, 101 - 106, 31.12.2024
Abdüllatif Karakaya
,
Tuğba Erçetin
,
Ulviye Acar Çevik
,
Yusuf Özkay
Abstract
In this study, 7 new thiazole derivatives were synthesized. Cholinesterase inhibition and antioxidant properties were examined to understand whether the synthesized compounds were anti-Alzheimer drug candidates. The antioxidant properties of these newly synthesized thiazole derivatives and their enzyme inhibition values for acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) were evaluated. According to the data, these substances inhibited the AChE and BuChE enzymes at deficient levels. Compound 2e showed the highest AChE inhibition effect with a value of 20.32 ± 0.005% at 50 µM concentration. Although high activity against BuChE was not observed, compound 2d was an exception with a value of 32.54 ± 0.021% at 50 µM concentration. Values that were comparable to the reference medication gallic acid were found when the antioxidant qualities were investigated using DPPH and ferric ion chelation studies. Ferrous ion-chelating and DPPH radical scavenging consistent with all of the previously reported information, the compounds’ antioxidant properties were very high, despite their modest cholinesterase enzyme inhibitory capabilities. In terms of AChE inhibition and antioxidant activity, respectively, compounds 2e and 2f were shown to be promising prospective agents among these compounds’.
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Year 2024,
Volume: 3 Issue: 3, 101 - 106, 31.12.2024
Abdüllatif Karakaya
,
Tuğba Erçetin
,
Ulviye Acar Çevik
,
Yusuf Özkay
References
- Wiloch MZ, Perez-Estebanez M, Baran N, Heras A, Jönsson-Niedziółka M, Colina A. Spectroelectrochemical studies of TDMQ20: A potential drug against Alzheimer’s disease. Bioelectrochem. (2025); 161: 108814. https://doi.org/10.1016/j.bioelechem.2024.108814.
- Lombardo S, Maskos U. Role of the nicotinic acetylcholine receptor in Alzheimer’s disease pathology and treatment. Neuropharmacol. (2015); 96: 255-262. https://doi.org/10.1016/j.neuropharm.2014.11.018.
- Karran E, Mercken M, Strooper B De. The amyloid cascade hypothesis for Alzheimer’s disease: An appraisal for the development of therapeutics. Nat Rev Drug Discov. (2011); 10: 698–712. https://doi.org/10.1038/nrd3505.
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- Karakaya A, Çevik UA, Erçetin T, Özkay Y, Kaplancıklı ZA. Synthesis of Imidazole-Thiazole Derivatives as Acetylcholinesterase and Butyrylcholinesterase Inhibitory Activities. Pharm Chem J. (2023); 57(9): 1439–43. https://doi.org/10.1007/s11094-023-03007-8.
- Ellman GL, Courtney KD, Andres Jr V, Featherstone RM. A new and rapid colorimetric determination of acetylcholinesterase activity. Biochem Pharmacol. (1961); 7(2): 88–95. https://doi.org/10.1016/0006-2952(61)90145-9.
- Dinis TCP, Madeira VMC, Almeida LM. Action of phenolic derivatives (acetaminophen, salicylate, and 5-aminosalicylate) as inhibitors of membrane lipid peroxidation and as peroxyl radical scavengers. Arch Biochem Biophys. (1994); 315(1): 161–9. https://doi.org/10.1006/abbi.1994.1485.
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