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    Determination of the inhibition profiles of pyrazolyl-thiazole derivatives against aldose reductase and ?-glycosidase and molecular docking studies
    (Wiley-V C H Verlag Gmbh, 2020) Demir, Yeliz; Taslimi, Parham; Kocyigit, Umit M.; Akkus, Musa; Ozaslan, Muhammet Serhat; Duran, Hatice Esra; Budak, Yakup
    Aldose reductase (AR) is the first and rate-limiting enzyme of the polyol pathway, which converts glucose to sorbitol in an NADPH-dependent reaction. alpha-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 alpha-glycosidase enzymes were investigated. All compounds showed a good inhibitory action against AR and alpha-glycosidase. Among these compounds, compound3dexhibited the best inhibition profiles against AR, with aK(i)value of 7.09 +/- 0.19 mu M, whereas compound3eshowed the lowest inhibition effects, with aK(i)value of 21.89 +/- 1.87 mu M. Also, all compounds showed efficient inhibition profiles against alpha-glycosidase, withK(i)values in the range of 0.43 +/- 0.06 to 2.30 +/- 0.48 mu M, whereas theK(i)value of acarbose was 12.60 +/- 0.78 mu M. Lastly, molecular modeling approaches were implemented to predict the binding affinities of compounds against AR and alpha-glycosidase. In addition, the ADME analysis of the molecules was performed.
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    Some old 2-(4-(Aryl)- thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7- tethanoisoindole-1,3(2H)-dione derivatives: Synthesis, inhibition effects and molecular docking studies on Aldose reductase and ?-Glycosidase
    (2021) Taslimi, Parham; Demir, Yeliz; Duran, Hatice Esra; Koçyiğit, Ü.Muhammet; Tuzun, Burak; Aslan, Osman Nuri; Ceylan, Mustafa
    Utilizing the simple chromatic techniques, Aldose reductase (AR) was derived from sheep liver. In addition, ?-glycosidase from Saccharomyces cerevisiae was used as the enzyme. It was determined the interactions between compounds and the enzymes. Molecular docking method used to compare biological activity values of molecules against enzymes. In the current study, the inhibition effect of synthetic isoindol-substitute thiazole derivatives (3a-f) on AR, and ?-glycosidase enzymes was studied. In the thiazole series, compound 3b (Ki: 9.70±4.72 ?M) showed a maximum inhibitory impact towards AR while compound 3f (Ki: 44.40±17.18 ?M) showed a lowest inhibitory impact towards AR. It was investigated potent inhibition profiles with Ki values in the range of 24.54±6.92–44.25±10.34 ?M against ?-glycosidase. Theoretical results were found consistent with experimental results. Acting as antidiabetic agents, these compounds have the potential to be the selective inhibitor of ?-glycosidase and AR enzymes. The biological activities of the studied molecules against AR and ?-glycosidase enzymes will be compared with molecular docking method. ADME analysis of the molecules will be done.
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    Some old 2-(4-(Aryl)- thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-tethanoisoindole-1,3(2H)-dione derivatives: Synthesis, inhibition effects and molecular docking studies on Aldose reductase and α-Glycosidase
    (Sivas Cumhuriyet Üniversitesi, 2021) Taslımı, Parham; Demir, Yeliz; Duran, Hatice Esra; Koçyiğit, Ümit Muhammet; Tüzün, Burak; Aslan, Osman Nuri; Ceylan, Mustafa
    Utilizing the simple chromatic techniques, Aldose reductase (AR) was derived from sheep liver. In addition, α-glycosidase from Saccharomyces cerevisiae was used as the enzyme. It was determined the interactions between compounds and the enzymes. Molecular docking method used to compare biological activity values of molecules against enzymes.In the current study, the inhibition effect of synthetic isoindol-substitute thiazole derivatives (3a-f) on AR, and α-glycosidase enzymes was studied. In the thiazole series, compound 3b (Ki: 9.70±4.72 M) showed a maximum inhibitory impact towards AR while compound 3f (Ki: 44.40±17.18 M) showed a lowest inhibitory impact towards AR. It was investigated potent inhibition profiles with Ki values in the range of 24.54±6.92–44.25±10.34 M against α-glycosidase. Theoretical results were found consistent with experimental results.Acting as antidiabetic agents, these compounds have the potential to be the selective inhibitor of α-glycosidase and AR enzymes. The biological activities of the studied molecules against AR and α-glycosidase enzymes will be compared with molecular docking method. ADME analysis of the molecules will be done.
  • Küçük Resim Yok
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    Synthesis, α-Glucosidase, α-Amylase, and Aldol Reductase Inhibitory Activity with Molecular Docking Study of Novel Imidazo[1,2-a]pyridine Derivatives
    (Amer Chemical Soc, 2024) Kaya, Betul; Cevik, Ulviye Acar; Ciftci, Bilge; Duran, Hatice Esra; Turkes, Cuneyt; Isik, Mesut; Bostanci, Hayrani Eren
    Inhibition ofaldose reductase (AR), alpha-glycosidase (alpha-GLY), and alpha-amylase (alpha-AMY) are some of the essential targets in diabetes mellitus (DM). Here, a series of imidazo[1,2-a]pyridine-based 1,3,4-thiadiazole derivatives (8a-k) were successfully synthesized and characterized using 1H NMR, 13C NMR, and HRMS spectroscopic techniques. The inhibition effects of the synthesized derivatives against AR, alpha-GLY, and alpha-AMY were evaluated using both in vitro and in silico methods. In vitro studies revealed that the derivatives (8a-k) showed significant inhibition activity. The results showed that the novel derivatives (8a-k) demonstrated potential inhibitory activity, with K I values covering the following ranges: 23.47 +/- 2.40 to 139.60 +/- 13.33 nM for AR and 6.09 +/- 0.37 to 119.80 +/- 12.31 mu M for alpha-GLY, with IC50 values 81.14 to 153.51 mu M for alpha-AMY. Furthermore, many of these compounds exhibited high inhibition activity, while some of them showed higher potency than the reference compounds. Molecular docking of the target compounds was carried out in the active sites of AR (PDB ID: 4JIR) and alpha-GLY (PDB ID: 5NN8).