2-Mercapto Benzothiazole Derivatives: As Potential Leads for the Diabetic Management

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Author(s): Saeed Ullah, Salma Mirza, Uzma Salar, Shafqat Hussain, Kulsoom Javaid, Khalid Mohammed Khan*, Ruqaiya Khalil, Atia Tul Wahab, Zaheer Ul-Haq, Shahnaz Perveen, M. Iqbal Choudhary.

Journal Name: Medicinal Chemistry

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Background: Results of our previous studies on antiglycation activity, and the non-cytotoxicity of 2-mercapto benzothiazoles, prompted us to further widen our investigation towards the identification of leads against diabetes mellitus.

Method: 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.

Keywords: 2-Mercapto benzothiazole; In vitro α-glucosidase inhibitory activity; Hyperglycemia; In silico studies

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(E-pub Ahead of Print)
DOI: 10.2174/1573406415666190612153150
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