Benzothiazole-thiadiazole hybrids as dual α-glucosidase and aldose reductase inhibitors: Synthesis, in vitro, and In Silico studies
Yazarlar (9)
Doç. Dr. Betül Kaya Türkiye
Prof. Dr. Ulviye Acar Çevik Türkiye
Nour El-Huda Daoud
Doç. Dr. Hatice Esra DURAN Kafkas Üniversitesi, Türkiye
Öğr. Gör. Bilge Çiftci Türkiye
Prof. Dr. Mesut Işık Bilecik Şeyh Edebali Üniversitesi, Türkiye
Doç. Dr. Hayrani Eren Bostancı Türkiye
Prof. Dr. Zafer Asım Kaplancıklı Türkiye
Prof. Dr. Şükrü Beydemir Anadolu 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 Dergi Bilgileri (2026) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 03-2026 |
| Cilt / Sayı / Sayfa | 1355 / 0 / 144995– | DOI | 10.1016/j.molstruc.2025.144995 |
| Makale Linki | https://doi.org/10.1016/j.molstruc.2025.144995 | ||
| UAK Araştırma Alanları |
Tıbbi Biyokimya
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| 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 | |
| Web of Science | 1 |
| Google Scholar | 1 |