Development of novel diaryl ether–phenolic Mannich Base derivatives with potent cholinesterase inhibition and low neuronal toxicity
Yazarlar (6)
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Pelin Tokalı
Kafkas Üniversitesi, Veteriner Fakültesi, Türkiye
Kafkas Üniversitesi, Veteriner Fakültesi, Türkiye
Doç. Dr. Ayşe Merve Şenol Sağlık Bilimleri Üniversitesi, Türkiye
Prof. Dr. Onur AKYILDIRIM Kafkas Üniversitesi, Türkiye
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Bioorganic Chemistry (Q1) | ||
| Dergi ISSN | 0045-2068 Dergi Bilgileri (2026) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 10-2026 |
| Cilt / Sayı / Sayfa | 181 / 1 / – | DOI | 10.1016/j.bioorg.2026.110354 |
| Makale Linki | https://doi.org/10.1016/j.bioorg.2026.110354 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| Alzheimer's disease (AD) is a progressive neurodegenerative disorder characterized by cholinergic dysfunction, making acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) attractive therapeutic targets. In the present study, twelve novel phenolic Mannich base-derived hydrazones incorporating a diaryl ether scaffold were rationally designed, synthesized, and evaluated as cholinesterase inhibitors. All synthesized compounds exhibited potent nanomolar inhibition against both cholinesterases, with K i values ranging from 24.27 to 98.56 nM for AChE and 28.68–148.41 nM for BChE. Compound 5 was identified as the most potent AChE inhibitor ( K i = 24.27 nM), whereas compound 6 showed the highest BChE inhibitory activity ( K i = 28.68 nM). Both compounds were considerably more potent than the reference inhibitors tacrine and donepezil. Enzyme kinetic studies revealed that all … |
| Anahtar Kelimeler |
| Acetylcholinesterase | Alzheimer's disease | Butyrylcholinesterase | Phenolic Mannich bases | SH-SY5Y |
Science Direct
Development of novel diaryl ether–phenolic Mannich Base derivatives with potent cholinesterase inhibition and low neuronal toxicity
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 1 |
| Scopus | 1 |
| Google Scholar | 3 |