Determination of the inhibition profiles of pyrazolyl–thiazolederivatives against aldose reductase and α‐glycosidase andmolecular docking studies
Yazarlar (13)
Yeliz Demir Ardahan Üniversitesi, Türkiye
Ümit Muhammet Koçyiğit Sivas Cumhuriyet Üniversitesi, Türkiye
Musa Akkuş
Muhammet Serhat Özarslan
Hatice Esra Duran Kafkas Üniversitesi, Türkiye
Prof. Dr. Yakup BUDAK Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Burak Tüzün Sivas Cumhuriyet Üniversitesi, Türkiye
Prof. Dr. Meliha Burcu GÜRDERE Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Mustafa CEYLAN Tokat Gaziosmanpaşa Üniversitesi, Türkiye
İlhami Gülçin Atatürk Üniversitesi, Türkiye
Şükrü Beydemir Anadolu Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | ARCHIV DER PHARMAZIE (Q4) | ||
| Dergi ISSN | 0365-6233 Wos Dergi Scopus Dergi | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 12-2020 |
| Cilt / Sayı / Sayfa | 353 / 12 / 2000118–0 | DOI | 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 Ki value of 7.09 ± 0.19 µM, whereas … |
| Anahtar Kelimeler |
| aldose reductase | enzyme inhibition | molecular docking | pyrazolyl-thiazole | α-glycosidase |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Google Scholar | 82 |
| Web of Science | 76 |