Benzothiazole-thiadiazole hybrids as dual α-glucosidase and aldose reductase inhibitors: Synthesis, in vitro, and In Silico studies
Yazarlar (9)
Türkiye
Türkiye
Doç. Dr. Hatice Esra DURAN
Kafkas Üniversitesi, Türkiye
Türkiye
Bilecik Şeyh Edebali Üniversitesi, Türkiye
Türkiye
Türkiye
Anadolu Üniversitesi, Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | Journal of Molecular Structure |
| Dergi ISSN | 0022-2860 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q2 |
| Makale Dili | İngilizce |
| Basım Tarihi | 01-2026 |
| Cilt No | 1355 |
| DOI Numarası | 10.1016/j.molstruc.2025.144995 |
| Makale Linki | https://doi.org/10.1016/j.molstruc.2025.144995 |
| Özet |
| The present study explores the synthesis, characterization, α-glucosidase and aldose reductase inhibitory activities of some novel benzothiazole-thiadiazole hybride compounds. All compounds exhibited a higher potential of aldose reductase (AR) inhibition (KI: 4.816 ± 0.342-19.47 ± 1.726 nM and IC50: 5.698-12.560 nM) compared to the reference inhibitor epalrestat (KI: 756.342 ± 52.874 nM, IC50: 787.142 nM), along with higher α-glucosidase (α-GLY) inhibitory activity (KI: 0.413 ± 0.032-20.971 ± 2.035 µM and IC50: 0.616-31.247 µM) relative to acarbose (KI: 119.43 ± 10.65 µM and IC50: 136.28 µM). Among the tested compounds, especially compounds 4a (KI: 4.816 ± 0.342 nM), 4b (KI: 6.244 ± 0.456 nM), and 4i (KI: 5.260 ± 0.386 nM) stand out as the most potent AR inhibitors while compounds 4b (KI: 1.166 ± 0.097 µM) and 4c (KI: 0.413 ± 0.032 µM) come forward as the strongest candidates for α-GLY inhibition … |
| Anahtar Kelimeler |
| 1,3,4-thiadiazole | & Acy;-glucosidase | ADMET | Aldose reductase | Benzothiazole | Diabetes mellitus | Molecular docking |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları |