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. 2016 Apr:65:100-9.
doi: 10.1016/j.bioorg.2016.02.004. Epub 2016 Feb 13.

Synthesis, α-glucosidase inhibitory, cytotoxicity and docking studies of 2-aryl-7-methylbenzimidazoles

Muhammad Taha  1 , Nor Hadiani Ismail  2 , Syahrul Imran  2 , Muhammad Helmi Mohamad  2 , Abdul Wadood  3 , Fazal Rahim  4 , Syed Muhammad Saad  5 , Ashfaq Ur Rehman  3 , Khalid Mohammed Khan  5
Affiliations

Synthesis, α-glucosidase inhibitory, cytotoxicity and docking studies of 2-aryl-7-methylbenzimidazoles

Muhammad Taha et al. Bioorg Chem. 2016 Apr.

Abstract

Benzimidazole analogs 1-27 were synthesized, characterized by EI-MS and (1)HNMR and their α-glucosidase inhibitory activities were found out experimentally. Compound 25, 19, 10 and 20 have best inhibitory activities with IC50 values 5.30±0.10, 16.10±0.10, 25.36±0.14 and 29.75±0.19 respectively against α-glucosidase. Compound 6 and 12 has no inhibitory activity against α-glucosidase enzyme among the series. Further studies showed that the compounds are not showing any cytotoxicity effect. The docking studies of the compounds as well as the experimental activities of the compounds correlated well. From the molecular docking studies, it was observed that the top ranked conformation of all the compounds fit well in the active site of the homology model of α-glucosidase.

Keywords: 4-Methylbenzimidazol; Antihyperglycemia; Cytotoxicity docking studies; Structure–activity relationship; α-glucosidase inhibitors.

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