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. 2016 Feb:64:29-36.
doi: 10.1016/j.bioorg.2015.11.006. Epub 2015 Nov 23.

Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies

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Benzimidazole derivatives as new α-glucosidase inhibitors and in silico studies

Nik Khairunissa Nik Abdullah Zawawi et al. Bioorg Chem. 2016 Feb.

Abstract

Newly synthesized benzimidazole hydrazone derivatives 1-26 were evaluated for their α-glucosidase inhibitory activity. Compounds 1-26 exhibited varying degrees of yeast α-glucosidase inhibitory activity with IC50 values between 8.40 ± 0.76 and 179.71 ± 1.11 μM when compared with standard acarbose. In this assay, seven compounds that showed highest inhibitory effects than the rest of benzimidazole series were identified. All the synthesized compounds were characterized by different spectroscopic methods adequately. We further evaluated the interaction of the active compounds with enzyme with the help of docking studies.

Keywords: Benzimidazole; Hydrazone; In silico studies; α-Glucosidase activity.

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