article · Pharmaceutics
A new series of hybrid benzimidazole urea compounds has been synthesised and evaluated for antioxidant properties and antidiabetic potential. Laboratory tests demonstrated that nearly all the synthesised molecules possessed moderate to strong antioxidant capabilities, with one specific variant showing notable activity across four standard testing methods. When assessed against key digestive enzymes involved in carbohydrate breakdown, namely alpha-amylase and alpha-glucosidase, several candidates displayed significant inhibitory effects. In particular, three specific compounds demonstrated inhibitory potency approaching that of the standard therapeutic drug acarbose. Complementary computational docking simulations confirmed that these molecules can bind effectively to the active sites of human pancreatic alpha-amylase and human lysosomal acid alpha-glucosidase. Together, the experimental and computational findings indicate that these novel chemical entities show promise as candidates for managing high blood sugar levels.
Managing blood glucose levels and combating oxidative stress are critical components of diabetes care. Therapies that simultaneously counteract oxidative damage and inhibit enzymes responsible for carbohydrate digestion could offer therapeutic benefits. Demonstrating that newly synthesised molecules achieve enzyme inhibition comparable to standard commercial agents provides a basis for creating alternative therapeutic options.
The research presents candidate molecules that could inform future pharmaceutical drug discovery programmes targeting diabetes management. Potential users include pharmaceutical developers and medicinal chemistry researchers seeking alternative small-molecule enzyme inhibitors. The work is at an early experimental stage, consisting strictly of chemical synthesis, computational docking, and in vitro enzyme inhibition assays, meaning extensive preclinical validation and safety testing remain necessary prior to any practical therapeutic application.
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A novel series of benzimidazole ureas 3a–h were elaborated using 2-(1H-benzoimidazol-2-yl) aniline 1 and the appropriate isocyanates 2a–h. The antioxidant and possible antidiabetic activities of the target benzimidazole-ureas 3a–h were evaluated. Almost all compounds 3a–h displayed strong to moderate antioxidant activities. When tested using the three antioxidant techniques, TAC, FRAP, and MCA, compounds 3b and 3c exhibited marked activity. The most active antioxidant compound in this family was compound 3g, which had excellent activity using four different methods: TAC, FRAP, DPPH-SA, and MCA. In vitro antidiabetic assays against α-amylase and α-glucosidase enzymes revealed that the majority of the compounds tested had good to moderate activity. The most favorable results were obtained with compounds 3c, 3e, and 3g, and analysis revealed that compounds 3c (IC50 = 18.65 ± 0.23 μM), 3e (IC50 = 20.7 ± 0.06 μM), and 3g (IC50 = 22.33 ± 0.12 μM) had good α-amylase inhibitory potential comparable to standard acarbose (IC50 = 14.21 ± 0.06 μM). Furthermore, the inhibitory effect of 3c (IC50 = 17.47 ± 0.03 μM), 3e (IC50 = 21.97 ± 0.19 μM), and 3g (IC50 = 23.01 ± 0.12 μM) on α-glucosidase was also comparable to acarbose (IC50 = 15.41 ± 0.32 μM). According to in silico molecular docking studies, compounds 3a–h had considerable affinity for the active sites of human lysosomal acid α-glucosidase (HLAG) and pancreatic α-amylase (HPA), indicating that the majority of the examined compounds had potential anti-hyperglycemic action.
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DOI: 10.3390/pharmaceutics15020457
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