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

Bioorganic Chemistry
Muhammad TahaKhalid Mohammed Khan

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.

References

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Citations

Jan 4, 2017·Bioorganic Chemistry·Nik Khairunissa Nik Abdullah ZawawiFazal Rahim
Jan 20, 2017·Journal of Enzyme Inhibition and Medicinal Chemistry·Jelena B Popović-DjordjevićTatjana P Stanojković
Jun 7, 2017·Chemical Biology & Drug Design·Alexander A SpasovYuri N Klimochkin
Nov 8, 2018·Chemical Biology & Drug Design·Arshad MehmoodChengtao Wang
Jun 23, 2020·Archiv der Pharmazie·Laxmi DeswalSuman Punia

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