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

ABSTRACT: A novel series of 2-substituted-4,6-diarylpyrimidines 6a-6t has been synthesized, characterized by ¹H-NMR, 13C-NMR and HRMS, and screened for in vitro ?-glucosidase inhibitory activity. The majority of the screened compounds possessed significant ?-glucosidase inhibitory activity with IC50 values ranging from 19.6 ± 0.21 to 38.9 ± 0.35 ?M, which is more potent than the positive control ?-glucosidase inhibitor acarbose (IC50 = 817.38 ± 6.27 ?M). Among them, 6j was found to be the most active compound against ?-glucosidase with an IC50 of 19.6 ± 0.21 ?M. In addition, molecular docking studies were carried out to explore the binding interactions of 2-substituted-4,6-diarylpyrimidine derivatives with ?-glucosidase.

SUBMITTER: Gong Z 

PROVIDER: S-EPMC6150375 | biostudies-other | 2017 Oct

REPOSITORIES: biostudies-other

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

Gong Zipeng Z   Xie Zhenzhen Z   Qiu Jie J   Wang Guangcheng G  

Molecules (Basel, Switzerland) 20171030 11

A novel series of 2-substituted-4,6-diarylpyrimidines <b>6a</b>-<b>6t</b> has been synthesized, characterized by ¹H-NMR, <sup>13</sup>C-NMR and HRMS, and screened for in vitro <i>α</i>-glucosidase inhibitory activity. The majority of the screened compounds possessed significant α-glucosidase inhibitory activity with IC<sub>50</sub> 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 (IC<sub>50</sub> = 817.38 ± 6.27 μM  ...[more]

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