Determination of the inhibition profiles of pyrazolyl–thiazole derivatives against aldose reductase and α‐glycosidase and molecular docking studies
Yazarlar (13)
Prof. Dr. Yeliz Demir Ardahan Üniversitesi, Türkiye
Parham Taslimi
Prof. Dr. Ümit Muhammet Koçyiğit Sivas Cumhuriyet Üniversitesi, Türkiye
Musa Akkuş
Doç. Dr. Muhammet Serhat Özaslan Ardahan Üniversitesi, Türkiye
Doç. Dr. Hatice Esra DURAN Kafkas Üniversitesi, Türkiye
Yakup Budak Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Burak Tüzün Sivas Cumhuriyet Üniversitesi, Türkiye
Meliha Burcu Gürdere Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Mustafa Ceylan Tokat Gaziosmanpaşa Üniversitesi, Türkiye
Prof. Dr. Seyithan Taysı Gaziantep Üniversitesi, Türkiye
Prof. Dr. İlhami Gülçin Atatürk Üniversitesi, Türkiye
Prof. Dr. Şükrü Beydemir Anadolu Üniversitesi, Türkiye
| Makale Türü | Özgün Makale (SSCI, AHCI, SCI, SCI-Exp dergilerinde yayınlanan tam makale) | ||
| Dergi Adı | ARCHIV DER PHARMAZIE (Q2) | ||
| Dergi ISSN | 0365-6233 Dergi Bilgileri (2020) | ||
| Dergi Tarandığı Indeksler | SCI-Expanded | ||
| Makale Dili | İngilizce | Basım Tarihi | 12-2020 |
| Kabul Tarihi | 11-07-2020 | Yayınlanma Tarihi | 06-08-2020 |
| Cilt / Sayı / Sayfa | 353 / 12 / 2000118–0 | DOI | 10.1002/ardp.202000118 |
| Makale Linki | http://dx.doi.org/10.1002/ardp.202000118 | ||
| UAK Araştırma Alanları |
Tıbbi Biyokimya
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| 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 | alpha-glycosidase |
BM Sürdürülebilir Kalkınma Amaçları
| Atıf Sayıları | |
| Web of Science | 78 |
| Google Scholar | 83 |