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Molecules 2017, 22(11), 1865; doi:10.3390/molecules22111865

Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors

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, Jishou University, Jishou 416000, China
*
Author to whom correspondence should be addressed.
Received: 30 September 2017 / Revised: 27 October 2017 / Accepted: 27 October 2017 / Published: 30 October 2017
(This article belongs to the Section Medicinal Chemistry)
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Abstract

A novel series of 2-substituted-4,6-diarylpyrimidines 6a6t has been synthesized, characterized by 1H-NMR, 13C-NMR and HRMS, and screened for in vitro α-glucosidase inhibitory activity. The majority of the screened compounds possessed significant α-glucosidase inhibitory activity with IC50 values ranging from 19.6 ± 0.21 to 38.9 ± 0.35 μM, which is more potent than the positive control α-glucosidase inhibitor acarbose (IC50 = 817.38 ± 6.27 μM). Among them, 6j was found to be the most active compound against α-glucosidase with an IC50 of 19.6 ± 0.21 μM. In addition, molecular docking studies were carried out to explore the binding interactions of 2-substituted-4,6-diarylpyrimidine derivatives with α-glucosidase. View Full-Text
Keywords: α-glucosidase; molecular docking; pyrimidine; chalcone α-glucosidase; molecular docking; pyrimidine; chalcone
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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.; Xie, Z.; Qiu, J.; Wang, G. Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors. Molecules 2017, 22, 1865.

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