In vitro and in silico studies of bis (indol-3-yl) methane derivatives as potential α-glucosidase and α-amylase inhibitors

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 5 g (IC(50): 7.54 ± 1.10 μM), 5e (IC(50): 9.00 ± 0.97 μM), and 5 h (IC(50): 9.57 ± 0.62 μM) presented strongest inhibitory activities against α-glucosidase, that were ∼ 30 times stronger than acarbose. Compounds 5 g (IC(50): 32.18 ± 1.66 µM), 5 h (IC(50): 31.47 ± 1.42 µM), and 5 s (IC(50): 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 5 g and 5 h HIGHLIGHTS: 1. A series of bis (indol-3-yl) methanes (BIMs) were synthesised and evaluated inhibitory activities against α-glucosidase and α-amylase. 2. Compound 5g exhibited promising activity (IC(50) = 7.54 ± 1.10 μM) against α-glucosidase. 3. Compound 5s exhibited promising activity (IC(50) = 30.91 ± 0.86 μM) against α-amylase. 4. In silico studies were performed to confirm the binding interactions of synthetic compounds with the enzyme active site.