AI Article Synopsis
- Benzimidazole analogs 1-27 were created and tested for their ability to inhibit the enzyme α-glucosidase, with compounds 25, 19, 10, and 20 showing the strongest inhibitory effects.
- Additionally, compounds 6 and 12 were found to have no effect on the enzyme, while the tested compounds exhibited no cytotoxicity.
- Molecular docking studies indicated that the best-fit conformations of these compounds align well with the active site of α-glucosidase, supporting the experimental findings.
Article 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.
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| http://dx.doi.org/10.1016/j.bioorg.2016.02.004 | DOI Listing |
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