| Yazarlar (9) |
Betül Kaya
Türkiye |
|
Ulviye Acar Çevik
Türkiye |
|
Bilge Çiftci
Türkiye |
Doç. Dr. Hatice Esra DURAN
Kafkas Üniversitesi, Türkiye |
|
Cüneyt Türkeş
Erzincan Binali Yıldırım Üniversitesi, Türkiye |
|
Mesut Işık
Bilecik Şeyh Edebali Üniversitesi, Türkiye |
|
Hayrani Eren Bostancı
Türkiye |
|
Zafer Asım Kaplancıklı
Türkiye |
|
Şükrü Beydemir
Anadolu Üniversitesi, Türkiye |
| Özet |
| Inhibition ofaldose reductase (AR), α-glycosidase (α-GLY), and α-amylase (α-AMY) are some of the essential targets in diabetes mellitus (DM). Here, a series of imidazo[1,2-]pyridine-based 1,3,4-thiadiazole derivatives (-) were successfully synthesized and characterized using H NMR, C NMR, and HRMS spectroscopic techniques. The inhibition effects of the synthesized derivatives against AR, α-GLY, and α-AMY were evaluated using both in vitro and in silico methods. In vitro studies revealed that the derivatives (-) showed significant inhibition activity. The results showed that the novel derivatives (-) demonstrated potential inhibitory activity, with values covering the following ranges: 23.47 ± 2.40 to 139.60 ± 13.33 nM for AR and 6.09 ± 0.37 to 119.80 ± 12.31 μM for α-GLY, with IC values 81.14 to 153.51 μM for α-AMY. Furthermore, many of these compounds exhibited high inhibition activity, while some of them showed higher potency than the reference compounds. Molecular docking of the target compounds was carried out in the active sites of AR (PDB ID: 4JIR) and α-GLY (PDB ID: 5NN8). |
| Anahtar Kelimeler |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | ACS Omega |
| Dergi ISSN | 2470-1343 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q2 |
| Makale Dili | Türkçe |
| Basım Tarihi | 10-2024 |
| Cilt No | 9 |
| Sayı | 42 |
| Sayfalar | 42905 / 42914 |
| Doi Numarası | 10.1021/acsomega.4c05619 |
| Makale Linki | https://doi.org/10.1021/acsomega.4c05619 |
| Atıf Sayıları | |
| WoS | 4 |
| Google Scholar | 5 |
