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    Effective ?-glycosidase inhibitors based on polyphenolic benzothiazole heterocycles
    (Academic Press Inc Elsevier Science, 2024) Sevimli, Esra; Seyhan, Gokce; Akkaya, Didem; Sari, Suat; Barut, Burak; Koksoy, Baybars
    alpha-Glycosidase inhibition is one of the main approaches to treat Diabetes mellitus. Polyphenolic moieties are known to be responsible for yielding exhibit potent alpha-glycosidase inhibitory effects. In addition, compounds containing benzothiazole and Schiff base functionalities were previously reported to show alpha-glycosidase inhibition. In this paper, the synthesis of seven new phloroglucinol-containing benzothiazole Schiff base derivatives through the reaction of 6-substituted-2-aminobenzothiazole compounds with 2,4,6-trihydroxybenzaldehyde using acetic acid as a catalyst was reported. The synthesized compounds were characterized using spectroscopic methods such as FT-IR, 1 H NMR, 13 C NMR, and elemental analysis. The synthesized compounds were evaluated for their inhibitory effects on alpha-glycosidase, compounds 3f and 3g were found to show significant inhibitory properties when compared to the positive control. The IC 50 values of 3f and 3g were calculated as 24.05 +/- 2.28 and 18.51 +/- 1.19 mu M, respectively. Kinetic studies revealed that compounds 3f and 3g exhibited uncompetitive mode of inhibition against alpha-glycosidase. Molecular modeling predicted druglikeness for the title compounds and underpinned the importance of phloroglucinol hydroxyls for interacting with the key residues of alpha-glycosidase.
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    ?-Glycosidase activity of novel coumarin-triazole-coumarin dyads
    (Tubitak Scientific & Technological Research Council Turkey, 2025) Sirin, Ersin; Sevimli, Esra; Seyhan, Gokce; Barut, Burak; Kaya, Yunus; Koksoy, Baybars
    Novel coumarin-triazole-coumarin dyads were synthesized and characterized, and their alpha-glycosidase inhibitory activities were evaluated spectrophotometrically. Compound 4e exhibited the most pronounced inhibitory effect, with an IC50value of 38.98 +/- 0.77 mu M. The IC50 values for 4d and 4a were 93.55 +/- 1.70 mu M and 95.04 +/- 3.55 mu M, respectively. The Lineweaver-Burk plot showed that 4e inhibited alpha-glycosidase in a mixed type. In addition, the Ki value obtained from the Dixon plot was 19.95 +/- 0.15 mu M for alpha-glycosidase.