Synthesis and evaluation of aldose reductase inhibition of new thiazolidine-quinazoline hybrids through in vitro and in silico approaches
Yazarlar (5)
Doç. Dr. Halil Şenol Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Doç. Dr. Namık Kılınç Iğdır Üniversitesi, Türkiye
Arş. Gör. Furkan Çakır Bezm-İ Âlem Vakıf Üniversitesi, Türkiye
Gürgün Albay
Iğdır Üniversitesi, Türkiye
Iğdır 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 | Computational Biology and Chemistry (Q1) | ||
| Dergi ISSN | 1476-9271 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 10-2025 |
| Cilt / Sayı / Sayfa | 118 / 1 / 108486–0 | DOI | 10.1016/j.compbiolchem.2025.108486 |
| Makale Linki | https://doi.org/10.1016/j.compbiolchem.2025.108486 | ||
| UAK Araştırma Alanları |
Organik Kimya
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| Özet |
| In this study, eleven novel quinazolin-4(3H)-one-thiazolidine-4-one hybrid compounds (1−11) were synthesized and evaluated for their in vitro aldose reductase (AR) inhibitory activity as potential therapeutics for diabetic complications. Structural characterization was performed using FT-IR, NMR, and HRMS techniques. The biological activity evaluation revealed that the nature of the substituents at the C2 position of the quinazoline ring significantly influenced AR inhibition. Compounds with aromatic or alicyclic groups (8−11) exhibited superior inhibitory potency, with compound 11, containing a thiophene ring, showing the strongest inhibition (IC50 = 10.19 µM), comparable to the standard quercetin. Molecular docking studies identified key interactions between the compounds and AR enzyme, including hydrogen bonds with Cys-298 and His-110, and π-π stacking with Trp-111. Notably, compound 11 … |
| Anahtar Kelimeler |
| Aldose reductase | Molecular docking | Molecular dynamics | Quinazonline | Thiazolidinone |
Science Direct
Synthesis and evaluation of aldose reductase inhibition of new thiazolidine-quinazoline hybrids through in vitro and in silico approaches
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 16 |
| Scopus | 15 |
| Google Scholar | 16 |