biostudies-literatureKhan IAHigher Education Commission of PakistanHigher Education Commission6012https://www.ebi.ac.uk/biostudies/studies/S-EPMC9501035biostudies-literatureUnknown27(18)The α-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. α-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)-1<i>H</i>-benzimidazol-3-ium chloride was synthesized and screened for its α-glucosidase inhibitory potential. Compounds <b>5d</b>, <b>5f</b>, <b>5g</b>, <b>5h</b> and <b>5k</b> exhibited better α-glucosidase inhibitions compared to the standard drug (acarbose IC₅₀ = 58.8 ± 0.012 µM) with IC₅₀ values of 15 ± 0.030, 19 ± 0.060, 25 ± 0.106, 21 ± 0.07 and 26 ± 0.035 µM, 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.Molecules (Basel, Switzerland)Synthesis of Novel <i>N</i>-Methylmorpholine-Substituted Benzimidazolium Salts as Potential α-Glucosidase Inhibitors.PMC9501035NRPU-5614Ashfaq UAAslam SKhan IAZaki MEAAl-Hussain SAAhmad MSaddique FAfalseSynthesis of Novel <i>N</i>-Methylmorpholine-Substituted Benzimidazolium Salts as Potential α-Glucosidase Inhibitors.The α-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. α-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)-1<i>H</i>-benzimidazol-3-ium chloride was synthesized and screened for its α-glucosidase inhibitory potential. Compounds <b>5d</b>, <b>5f</b>, <b>5g</b>, <b>5h</b> and <b>5k</b> exhibited better α-glucosidase inhibitions compared to the standard drug (acarbose IC₅₀ = 58.8 ± 0.012 µM) with IC₅₀ values of 15 ± 0.030, 19 ± 0.060, 25 ± 0.106, 21 ± 0.07 and 26 ± 0.035 µM, 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.2022-01-01T00:00:00Z2022 Sep2026-04-08T11:48:19.094Z2025-02-19T00:44:20.402ZS-EPMC95010353614475010.3390/molecules27186012