Determination of the inhibition profiles of pyrazolyl–thiazolederivatives against aldose reductase and α‐glycosidase andmolecular docking studies
Yazarlar (13)
Ardahan Üniversitesi, Türkiye
Sivas Cumhuriyet Üniversitesi, Türkiye
Ardahan Üniversitesi, Türkiye
Kafkas Üniversitesi, Türkiye
Prof. Dr. Yakup BUDAK
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Sivas Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Meliha Burcu GÜRDERE
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN
Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Atatürk Üniversitesi, Türkiye
Anadolu Üniversitesi, Türkiye
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale |
| Dergi Adı | ARCHIV DER PHARMAZIE |
| Dergi ISSN | 0365-6233 Wos Dergi Scopus Dergi |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q4 |
| Makale Dili | İngilizce |
| Basım Tarihi | 12-2020 |
| Cilt No | 353 |
| Sayı | 12 |
| DOI Numarası | 10.1002/ardp.202000118 |
| Özet |
| Aldose reductase (AR) is the first and rate-limiting enzyme of the polyol pathway, which converts glucose to sorbitol in an NADPH-dependent reaction. α-Glycosidase breaks down starch and disaccharides to glucose. Hence, inhibition of these enzymes can be regarded a considerable approach in the treatment of diabetic complications. AR was purified from sheep liver using simple chromatographic methods. The inhibitory effects of pyrazolyl-thiazoles ((3aR,4S,7R,7aS)-2-(4-{1-[4-(4-bromophenyl)thiazol-2-yl]-5-(aryl)-4,5-dihydro-1H-pyrazol-3-yl}phenyl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives; 3a-i) on AR and α-glycosidase enzymes were investigated. All compounds showed a good inhibitory action against AR and α-glycosidase. Among these compounds, compound 3d exhibited the best inhibition profiles against AR, with a K value of 7.09 ± 0.19 µM, whereas compound 3e showed the lowest inhibition effects, with a K value of 21.89 ± 1.87 µM. Also, all compounds showed efficient inhibition profiles against α-glycosidase, with K values in the range of 0.43 ± 0.06 to 2.30 ± 0.48 µM, whereas the K value of acarbose was 12.60 ± 0.78 µM. Lastly, molecular modeling approaches were implemented to predict the binding affinities of compounds against AR and α-glycosidase. In addition, the ADME analysis of the molecules was performed. |
| Anahtar Kelimeler |
| aldose reductase | enzyme inhibition | molecular docking | pyrazolyl-thiazole | α-glycosidase |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| WoS | 74 |
| Google Scholar | 80 |