Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

İrem Bozbey; Gülce Taşkor Önel; Burçin Türkmenoğlu; Şule Gürsoy; Esra Dilek; Muhammed Ergün; Azime Berna Özçelik; Mehtap Uysal

Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme

Abstract

Alzheimer's disease is a neurological disease characterized by the destruction of brain cells. In this disease, which causes a decrease in thought, memory and behavioral functions, the symptoms appear gradually with age. In this study, inhibition of acetylcholinesterase enzyme which is an important target in accordance with the cholinergic hypothesis, was studied. New 3(2H)pyridazinone-triazole derivatives were synthesized, confirmed by 1H-NMR, 13CNMR, HRMS analysis and their IC50 and Ki values were studied. The inhibition constants (Ki) of the compounds against the AChE enzyme ranged from 2.35 ± 0.18 to 5.15 ± 0.46 μM. The compound with the best inhibitory properties was compound 6d with a Ki value of 2.35 ± 0.18 μM. In addition, to support the experimental data, molecular docking studies were carried out with 6b, 6d, 6e and 6f compounds with AChE crystal structure (PDB ID:4M0E).

Keywords

References

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Details

Primary Language

English

Subjects

Pharmaceutical Biochemistry, Pharmaceutical Chemistry

Journal Section

Research Article

Authors

İrem Bozbey ^* This is me
0000-0002-9290-938X
Türkiye

Gülce Taşkor Önel
0000-0002-9375-2329
Türkiye

Burçin Türkmenoğlu
Türkiye

Şule Gürsoy
0000-0001-5236-5974
Türkiye

Esra Dilek
0000-0002-3629-5168
Türkiye

Muhammed Ergün This is me
0000-0002-7231-5285
Türkiye

Azime Berna Özçelik
0000-0002-3160-5753
Türkiye

Mehtap Uysal
Türkiye

Publication Date

June 28, 2025

Submission Date

March 30, 2022

Acceptance Date

May 27, 2022

Published in Issue

Year 2022 Volume: 26 Number: 5

IZ

https://izlik.org/JA57LK27HS

Cite

RIS / Bibtex

APA

Bozbey, İ., Taşkor Önel, G., Türkmenoğlu, B., Gürsoy, Ş., Dilek, E., Ergün, M., Özçelik, A. B., & Uysal, M. (2025). Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme. Journal of Research in Pharmacy, 26(5), 1461-1471. https://izlik.org/JA57LK27HS

AMA

1.Bozbey İ, Taşkor Önel G, Türkmenoğlu B, et al. Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme. J. Res. Pharm. 2025;26(5):1461-1471. https://izlik.org/JA57LK27HS

Chicago

Bozbey, İrem, Gülce Taşkor Önel, Burçin Türkmenoğlu, et al. 2025. “Inhibitory Effects of Novel 3(2H)pyridazinone-Triazole Derivatives Against Acetylcholinesterase Enzyme”. Journal of Research in Pharmacy 26 (5): 1461-71. https://izlik.org/JA57LK27HS.

EndNote

Bozbey İ, Taşkor Önel G, Türkmenoğlu B, Gürsoy Ş, Dilek E, Ergün M, Özçelik AB, Uysal M (June 1, 2025) Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme. Journal of Research in Pharmacy 26 5 1461–1471.

IEEE

[1]İ. Bozbey et al., “Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme”, J. Res. Pharm., vol. 26, no. 5, pp. 1461–1471, June 2025, [Online]. Available: https://izlik.org/JA57LK27HS

ISNAD

Bozbey, İrem - Taşkor Önel, Gülce - Türkmenoğlu, Burçin - Gürsoy, Şule - Dilek, Esra - Ergün, Muhammed - Özçelik, Azime Berna - Uysal, Mehtap. “Inhibitory Effects of Novel 3(2H)pyridazinone-Triazole Derivatives Against Acetylcholinesterase Enzyme”. Journal of Research in Pharmacy 26/5 (June 1, 2025): 1461-1471. https://izlik.org/JA57LK27HS.

JAMA

1.Bozbey İ, Taşkor Önel G, Türkmenoğlu B, Gürsoy Ş, Dilek E, Ergün M, Özçelik AB, Uysal M. Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme. J. Res. Pharm. 2025;26:1461–1471.

MLA

Bozbey, İrem, et al. “Inhibitory Effects of Novel 3(2H)pyridazinone-Triazole Derivatives Against Acetylcholinesterase Enzyme”. Journal of Research in Pharmacy, vol. 26, no. 5, June 2025, pp. 1461-7, https://izlik.org/JA57LK27HS.

Vancouver

1.İrem Bozbey, Gülce Taşkor Önel, Burçin Türkmenoğlu, Şule Gürsoy, Esra Dilek, Muhammed Ergün, Azime Berna Özçelik, Mehtap Uysal. Inhibitory effects of novel 3(2H)pyridazinone-triazole derivatives against acetylcholinesterase enzyme. J. Res. Pharm. [Internet]. 2025 Jun. 1;26(5):1461-7. Available from: https://izlik.org/JA57LK27HS