Aldose reductase inhibition properties of novel thiazolidin-2,4-diones: In vitro and in silico approach for the treatment of diabetes-related complications
Yazarlar (7)
Doç. Dr. Feyzi Sinan TOKALI Kafkas Üniversitesi, Türkiye
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Arş. Gör. Şeyma Ateşoğlu Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Pelin Tokalı
Kafkas Üniversitesi, Veteriner Fakültesi, Türkiye
Kafkas Üniversitesi, Veteriner Fakültesi, Türkiye
Arş. Gör. Furkan Çakır Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Prof. Dr. Fahri Akbaş Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | Journal of Molecular Liquids (Q1) | ||
| Dergi ISSN | 0167-7322 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 04-2025 |
| Cilt / Sayı / Sayfa | 426 / 1 / – | DOI | 10.1016/j.molliq.2025.127487 |
| Makale Linki | https://doi.org/10.1016/j.molliq.2025.127487 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| The inhibition of aldose reductase (ALR2) presents a promising strategy for mitigating diabetes-related complications. In this study, eighteen novel thiazolidin-2,4-dione derivatives were synthesized and evaluated for their ALR2 inhibitory activity, with several exhibiting superior inhibition compared to the standard inhibitor epalrestat (EPR). Among them, compound 11 (4-trifluoromethylbenzene substituted) emerged as the most potent competitive inhibitor (Ki = 0.051 µM), demonstrating 19-fold higher activity than EPR. Molecular docking and molecular dynamics simulations further highlighted compound 11’s stable binding and key interactions with ALR2 active site residues, including Trp-111 and Tyr-209. Cytotoxicity assays performed on healthy cell lines (HUVEC and BEAS-B2) revealed that the tested compounds were non-toxic at inhibitory concentrations, with compound 3 (isovanillin substituted) exhibiting the … |
| Anahtar Kelimeler |
| Cytotoxicity | Diabetes | Diabetes-related complications aldose reductase | Thiazolidin-2,4-dion |
Science Direct
Aldose reductase inhibition properties of novel thiazolidin-2,4-diones: In vitro and in silico approach for the treatment of diabetes-related complications
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Scopus | 31 |
| Google Scholar | 34 |