Biological effects of bis-hydrazone compounds bearing isovanillin moiety on the aldose reductase
Yazarlar (8)
Doç. Dr. Gönül Yapar Türkiye
Doç. Dr. Hatice Esra DURAN Kafkas Üniversitesi, Türkiye
Doç. Dr. Nebih Lolak Türkiye
Doç. Dr. Süleyman Akocak Türkiye
Prof. Dr. Cüneyt Türkeş Türkiye
Prof. Dr. Mustafa Durgun Türkiye
Prof. Dr. Mesut Işık Bilecik Şeyh Edebali Üniversitesi, Türkiye
Prof. Dr. Şükrü Beydemir Anadolu Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | BIOORGANIC CHEMISTRY (Q1) | ||
| Dergi ISSN | 0045-2068 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | Türkçe | Basım Tarihi | 12-2021 |
| Kabul Tarihi | – | Yayınlanma Tarihi | 01-12-2021 |
| Cilt / Sayı / Sayfa | 117 / 0 / 105473–0 | DOI | 10.1016/j.bioorg.2021.105473 |
| Makale Linki | http://dx.doi.org/10.1016/j.bioorg.2021.105473 | ||
| UAK Araştırma Alanları |
Tıbbi Biyokimya
|
||
| Özet |
| Aldose reductase (ALR2), one of the metabolically important enzymes, catalyzes the formation of sorbitol from glucose in the polyol pathway. ALR2 inhibition is required to prevent diabetic complications. In the present study, the novel bis-hydrazone compounds bearing isovanillin moiety (GY1-12) were synthesized, and various chromatographic methods were applied to purify the ALR2 enzyme. Afterward, the inhibitory effect of the synthesized compounds on the ALR2 was screened in vitro. All the novel bis-hydrazones demonstrated activity in nanomolar levels as AR inhibitors with IC50 and KI values in the range of 12.55–35.04 nM, and 13.38–88.21 nM, respectively. Compounds GY-11, GY-7, and GY-5 against ALR2 were identified as the highly potent inhibitors, respectively, and were superior to the standard drug, epalrestat. Moreover, a comprehensive ligand-receptor interactions prediction was performed using … |
| Anahtar Kelimeler |
| Aldose reductase | Bis-hydrazones | Epalrestat | In silico study | ADME-Tox |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 66 |
| Google Scholar | 78 |