Novel triazole-based N-acetyl schiff bases: Synthesis, computational analysis, and acetylcholinesterase and butyrylcholinesterase inhibitory potential for Alzheimer's disease
Yazarlar (8)
Doç. Dr. Hilal MEDETALİBEYOĞLU Kafkas Üniversitesi, Türkiye
Prof. Dr. Burak Tüzün Cumhuriyet Üniversitesi, Türkiye
Dr. Öğr. Üyesi Abdurrahman Atalay Avrasya Üniversitesi, Türkiye
Ahmet Buğra Ortaakarsu
Gazi Üniversitesi, Türkiye
Gazi Üniversitesi, Türkiye
Dr. Öğr. Üyesi Rüya Kaya Aǧrı İbrahim Çeçen Üniversitesi, Türkiye
Doç. Dr. Sevda MANAP Kafkas Üniversitesi, Türkiye
Doç. Dr. Onur AKYILDIRIM Kafkas Üniversitesi, Türkiye
Prof. Dr. Haydar YÜKSEK Kafkas Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Journal of Molecular Structure (Q2) | ||
| Dergi ISSN | 0022-2860 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 12-2025 |
| Cilt / Sayı / Sayfa | 1347 / 1 / 1–20 | DOI | 10.1016/j.molstruc.2025.143176 |
| Makale Linki | https://doi.org/10.1016/j.molstruc.2025.143176 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| In the pursuit of novel therapeutic agents against Alzheimer's disease (AD), six N-acetyl Schiff base derivatives (F1-6), featuring a 1,2,4-triazole scaffold and sulfonate ester functionalities, were rationally designed, synthesized, and subjected to comprehensive biological and computational evaluation. Structural characterization was confirmed through FT-IR, UV-Vis, and NMR spectroscopy. Biological activity against acetylcholinesterase (AChE) and butyrylcholinesterase (BChE)—two critical enzymes in AD pathology—was assessed. Among the tested compounds, F2 and F5 demonstrated the most promising dual inhibitory profiles. F2 showed IC50 values of 3.05 µM (AChE) and 4.74 µM (BChE), with Ki values of 0.67 µM and 2.14 µM, respectively, indicating notable selectivity toward AChE (selectivity index, SI = 3.19). In contrast, F5 exhibited potent, balanced inhibition across both enzymes, with IC50 values of 2 … |
| Anahtar Kelimeler |
| 1,2,4-triazole | Acetylcholinesterase | Alzheimer's disease | Butyrylcholinesterase | Schiff bases |
Science Direct
Novel triazole-based N-acetyl schiff bases: Synthesis, computational analysis, and acetylcholinesterase and butyrylcholinesterase inhibitory potential for Alzheimer's disease
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 4 |
| Scopus | 4 |
| Google Scholar | 4 |