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Molecules 2017, 22(9), 1555; doi:10.3390/molecules22091555

Synthesis, In Vitro α-Glucosidase Inhibitory Activity and Molecular Docking Studies of Novel Benzothiazole-Triazole Derivatives

Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guizhou Medical University, Beijing Road, Guiyang 550004, China
School of Pharmacy, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China
National Engineering Research Center of Miao’s Medicines, 4 Beijing Road, Guiyang 550004, China
College of Chemistry and Chemical Engineering, Hunan Engineering Laboratory for Analyse and Drugs Development of Ethnomedicine in Wuling Mountains, Jishou University, Jishou 416000, China
Authors to whom correspondence should be addressed.
Received: 29 August 2017 / Accepted: 13 September 2017 / Published: 15 September 2017
(This article belongs to the Section Medicinal Chemistry)
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Benzothiazole-triazole derivatives 6a–6s have been synthesized and characterized by 1HNMR and 13C-NMR. All synthetic compounds were screened for their in vitro α-glucosidase inhibitory activity by using Baker’s yeast α-glucosidase enzyme. The majority of compounds exhibited a varying degree of α-glucosidase inhibitory activity with IC50 values between 20.7 and 61.1 μM when compared with standard acarbose (IC50 = 817.38 μM). Among the series, compound 6s (IC50 = 20.7 μM) bearing a chlorine group at the 5-position of the benzothiazole ring and a tertbutyl group at the para position of the phenyl ring, was found to be the most active compound. Preliminary structure-activity relationships were established. Molecular docking studies were performed to predict the binding interaction of the compounds in the binding pocket of the enzyme. View Full-Text
Keywords: benzothiazole; triazole; α-glucosidase; molecular docking benzothiazole; triazole; α-glucosidase; molecular docking

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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Gong, Z.; Peng, Y.; Qiu, J.; Cao, A.; Wang, G.; Peng, Z. Synthesis, In Vitro α-Glucosidase Inhibitory Activity and Molecular Docking Studies of Novel Benzothiazole-Triazole Derivatives. Molecules 2017, 22, 1555.

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