| Yazarlar (10) |
Betul Kaya
|
|
Ulviye Acar Cevik
|
|
Adem Necip
|
Doç. Dr. Hatice Esra DURAN
Kafkas Üniversitesi, Türkiye |
|
Bilge Ciftci
|
|
Mesut Isik
|
|
Pervin Soyer
|
|
Hayrani Eren Bostanci
|
|
Zafer Asim Kaplancikli
|
|
Sukru Beydemir
|
| Özet |
| We have developed new 1,3,4-thiadiazole derivatives and examined their ability to inhibit aldose reductase and α-glucosidase. All of the members of the series showed a higher potential of aldose reductase inhibition ( : 15.39 ± 1.61-176.50 ± 10.69 nM and IC: 20.16 ± 1.07-175.40 ± 6.97 nM) compared to the reference inhibitor epalrestat ( : 837.70 ± 53.87 nM, IC: 265.00 ± 2.26 nM). Furthermore, compounds , , , , , , and showed significantly higher inhibitory activity ( : 4.48 ± 0.25 μM-15.86 ± 0.92 μM and IC: 4.68 ± 0.23 μM-34.65 ± 1.78 μM) toward α-glucosidase compared to the reference acarbose ( : 21.52 ± 2.72 μM, IC: 132.51 ± 9.86 μM). Molecular docking studies confirmed that the most potent inhibitor of α-GLY, compound ( : 4.48 ± 0.25 μM), interacts with the target protein 5NN8 through hydrogen bonds as in acarbose. On the other hand, compounds ( : 15.39 ± 1.61 nM) and ( : 23.86 ± 2.41 nM), the most potent inhibitors for AR, establish hydrogen bonds with the target protein 4JIR like epalrestat. ADME/T analysis was performed to predict their drug-like properties. A cytotoxicity study was carried out with the L929 fibroblast cell line , revealing that all of the synthesized compounds were noncytotoxic. Furthermore, AMES test has been added to show the low mutagenic potential of the compounds and . |
| Anahtar Kelimeler |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | ESCI dergilerinde yayımlanan tam makale |
| Dergi Adı | ACS OMEGA |
| Dergi ISSN | 2470-1343 Wos Dergi Scopus Dergi |
| Makale Dili | İngilizce |
| Basım Tarihi | 05-2025 |
| Doi Numarası | 10.1021/acsomega.5c00566 |
| Atıf Sayıları |
