| Yazarlar |
Yeliz Demir
Ardahan Üniversitesi, Türkiye |
|
Parham Taslimi
Türkiye |
|
Ümit Muhammet Koçyiğit
Sivas Cumhuriyet Üniversitesi, Türkiye |
|
Musa Akkuş
Türkiye |
|
Muhammet Serhat Özaslan
Ardahan Üniversitesi, Türkiye |
Doç. Dr. Hatice Esra DURAN
Kafkas Üniversitesi, Türkiye |
|
Yakup Budak
Tokat Gaziosmanpaşa Üniversitesi, Türkiye |
|
Burak Tüzün
Sivas Cumhuriyet Üniversitesi, Türkiye |
|
Meliha Burcu Gürdere
Tokat Gaziosmanpaşa Üniversitesi, Türkiye |
|
Mustafa Ceylan
Tokat Gaziosmanpaşa Üniversitesi, Türkiye |
|
Seyithan Taysı
Gaziantep Üniversitesi, Türkiye |
|
İlhami Gülçin
Atatürk Üniversitesi, Türkiye |
|
Şükrü Beydemir
Anadolu Üniversitesi, Türkiye |
| 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 | alpha-glycosidase |
| Makale Türü | Özgün Makale |
| Makale Alt Türü | SSCI, AHCI, SCI, SCI-Exp dergilerinde yayımlanan tam makale |
| Dergi Adı | ARCHIV DER PHARMAZIE |
| Dergi ISSN | 0365-6233 |
| Dergi Tarandığı Indeksler | SCI-Expanded |
| Dergi Grubu | Q2 |
| Makale Dili | İngilizce |
| Basım Tarihi | 12-2020 |
| Cilt No | 353 |
| Sayı | 12 |
| Sayfalar | 2000118 / |
| Doi Numarası | 10.1002/ardp.202000118 |
| Makale Linki | http://dx.doi.org/10.1002/ardp.202000118 |
| Atıf Sayıları | |
| WoS | 64 |
| Google Scholar | 70 |
