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  • Title: 2-Mercapto Benzothiazole Derivatives: As Potential Leads for the Diabetic Management.
    Author: Ullah S, Mirza S, Salar U, Hussain S, Javaid K, Khan KM, Khalil R, Atia-Tul-Wahab, Ul-Haq Z, Perveen S, Choudhary MI.
    Journal: Med Chem; 2020; 16(6):826-840. PubMed ID: 31195949.
    Abstract:
    BACKGROUND: Results of our previous studies on antiglycation activity, and the noncytotoxicity of 2-mercapto benzothiazoles, encouraged us to further widen our investigation towards the identification of leads against diabetes mellitus. METHODS: 33 derivatives of 2-mercapto benzothiazoles 1-33 were evaluated for in vitro α- glucosidase inhibitory activity. Mode of inhibition was deduced by kinetic studies. To predict the interactions of 2-mercapto benzothiazole derivatives 1-33 with the binding pocket of α-glucosidase enzyme, molecular docking studies were performed on the selected inhibitors. RESULTS: Compounds 2-4, 6-7, 9-26, 28 and 30 showed many folds potent α-glucosidase inhibitory activity in the range of IC50 = 31.21-208.63 μM, as compared to the standard drug acarbose (IC50 = 875.75 ± 2.08 μM). It was important to note that except derivative 28, all other derivatives were also found previously to have antiglycating potential in the range of IC50 = 187.12-707.21 μM. CONCLUSION: A number of compounds were identified as dual nature as antiglycating agent and α- glucosidase inhibitors. These compounds may serve as potential lead candidates for the management of diabetes mellitus.
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