Abstract
The alpha-glucosidase enzyme, located in the brush border of the small intestine, is responsible for overall glycemic control in the body. It hydrolyses the 1,4-linkage in the carbohydrates to form blood-absorbable monosaccharides that ultimately increase the blood glucose level. alpha-Glucosidase inhibitors (AGIs) can reduce hydrolytic activity and help to control type 2 diabetes. Aiming to achieve this, a novel series of 1-benzyl-3-((2-substitutedphenyl)amino)-2-oxoethyl)-2-(morpholinomethyl)-1H-benzimidazol-3-ium chloride was synthesized and screened for its alpha-glucosidase inhibitory potential. Compounds 5d, 5f, 5g, 5h and 5k exhibited better alpha-glucosidase inhibitions compared to the standard drug (acarbose IC50 = 58.8 +/- 0.012 mu M) with IC50 values of 15 +/- 0.030, 19 +/- 0.060, 25 +/- 0.106, 21 +/- 0.07 and 26 +/- 0.035 mu M, respectively. Furthermore, the molecular docking studies explored the mechanism of enzyme inhibitions by different 1,2,3-trisubstituted benzimidazolium salts via significant ligand-receptor interactions.