In this paper, bis (indol-3-yl) methanes (BIMs) were synthesised and evaluated for their inhibitory activity against α-glucosidase and α-amylase. All synthesised compounds showed potential α-glucosidase and α-amylase inhibitory activities. Compounds (IC: 7.54 ± 1.10 μM), (IC: 9.00 ± 0.97 μM), and (IC: 9.57 ± 0.62 μM) presented strongest inhibitory activities against α-glucosidase, that were ∼ 30 times stronger than acarbose. Compounds (IC: 32.18 ± 1.66 µM), (IC: 31.47 ± 1.42 µM), and (IC: 30.91 ± 0.86 µM) showed strongest inhibitory activities towards α-amylase, ∼ 2.5 times stronger than acarbose. The mechanisms and docking simulation of the compounds were also studied. Compounds and exhibited bifunctional inhibitory activity against these two enzymes. Furthermore, compounds showed no toxicity against 3T3-L1 cells and HepG2 cells.HighlightsA series of bis (indol-3-yl) methanes (BIMs) were synthesised and evaluated inhibitory activities against -glucosidase and α-amylase.Compound exhibited promising activity (IC = 7.54 ± 1.10 μM) against -glucosidase.Compound exhibited promising activity (IC = 30.91 ± 0.86 μM) against α-amylase.In silico studies were performed to confirm the binding interactions of synthetic compounds with the enzyme active site.
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http://dx.doi.org/10.1080/14756366.2021.1971976 | DOI Listing |
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