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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.
  • Küçük Resim Yok
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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.
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    Synthesis and Carbonic Anhydrase Inhibition of Novel 2-(4-(Aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione Derivatives
    (WILEY-V C H VERLAG GMBH, 2016) Kocyigit, Umit M.; Aslan, Osman Nuri; Gulcin, Ilhami; Temel, Yusuf; Ceylan, Mustafa
    Carbonic anhydrase (CA, EC 4.2.1.1) is a member of the metalloenzyme family. It catalyzes the rapid conversion of carbon dioxide (CO2) and water to bicarbonate (HCO3-) and protons (H+) and also plays an important role in biochemical and physiological processes. In this study, a number of novel 2-(4-(aryl)thiazole-2-yl)-3a,4,7,7a-tetrahydro-1H-4,7-methanoisoindole-1,3(2H)-dione derivatives were synthesized and evaluated for their inhibitory characteristics against the human CA isoenzymes I and II (hCA I and hCA II). The structures of the new molecules 8a-i were confirmed by means of IR, H-1 NMR, C-13 NMR, and elemental analysis. These compounds exhibited excellent inhibitory effects, in the low nanomolar range, with K-i values in the range of 27.07-37.80 nM against hCA I and in the range of 11.80-25.81nM against hCA II. Our findings suggest that the new isoindolylthiazole derivatives have superior inhibitory effect over acetazolamide (AZA), which is used as clinical CA inhibitor with K-i values of 34.50 and 28.93nM against the hCA I and hCA II isoenzymes, respectively.