Chiral Anthranilic Amides as Potential Cholinesterase Inhibitors: Synthesis, Bioactivity Assessment, and Molecular Modeling
Yazarlar (4)
Doç. Dr. Turgay TUNÇ Kırşehir Ahi Evran Üniversitesi, Türkiye
Namık Kılınç Iğdır Üniversitesi, Türkiye
Prof. Dr. Nadir DEMİREL Kırşehir Ahi Evran Üniversitesi, Türkiye
Prof. Dr. Zuhal ALIM Kırşehir Ahi Evran Üniversitesi, Türkiye
| Makale Türü |
Özgün Makale
(SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale)
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| Dergi Adı | Chemistry and Biodiversity (Q3) | ||
| Dergi ISSN | 1612-1872 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 01-2025 |
| Kabul Tarihi | 12-04-2026 | Yayınlanma Tarihi | – |
| Cilt / Sayı / Sayfa | 22 / 11 / – | DOI | 10.1002/cbdv.202500974 |
| Makale Linki | https://doi.org/10.1002/cbdv.202500974 | ||
| Özet |
| Inhibitors of acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) are central therapeutic targets for Alzheimer's disease (AD). In this study, novel chiral anthranilic amide derivatives (5a–5d, 7a, and 7b) were synthesized from chiral amines and were characterized by 1H, 13C NMR, LC–MS, and IR, then inhibitory effect of 5a–5d, 7a, and 7b on AChE/BChE activity was investigated by in vitro inhibition and in silico studies. For AChE, IC50 values of 5a–5d, 7a, and 7b were found to be 70, 63.64, 53.85, 36.84, 17.07, and 17.5 nM, respectively. For BChE, IC50 values of 5a–5d, 7a, and 7b were found as 46.66 µM, 33.33 µM, 116.6 µM, 233.3 µM, 175 nM and, 116.6 nM, respectively. All compounds had better inhibition effects against AChE than BChE. The enantioselective inhibition was observed in the compounds 5a–5d. For AChE, the S‐enantiomers exhibited stronger inhibition than the R‐enantiomers … |
| Anahtar Kelimeler |
| acetylcholinesterase | butyrylcholinesterase | chiral anthranilic amide | inhibition | molecular docking |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Google Scholar | 1 |
| Web of Science | 1 |