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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

1
Provincial Key Laboratory of Pharmaceutics in Guizhou Province, Guizhou Medical University, Beijing Road, Guiyang 550004, China
2
School of Pharmacy, Guizhou Medical University, 4 Beijing Road, Guiyang 550004, China
3
National Engineering Research Center of Miao’s Medicines, 4 Beijing Road, Guiyang 550004, China
4
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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Abstract

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
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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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