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- Title
Synthesis of Novel N -Methylmorpholine-Substituted Benzimidazolium Salts as Potential α-Glucosidase Inhibitors.
- Authors
Khan, Imran Ahmad; Saddique, Furqan Ahmad; Aslam, Sana; Ashfaq, Usman Ali; Ahmad, Matloob; Al-Hussain, Sami A.; Zaki, Magdi E. A.
- Abstract
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)-1H-benzimidazol-3-ium chloride was synthesized and screened for its α-glucosidase inhibitory potential. Compounds 5d, 5f, 5g, 5h and 5k 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.
- Subjects
ALPHA-glucosidases; GLYCEMIC control; TYPE 2 diabetes; MOLECULAR docking; SALTS; BLOOD sugar
- Publication
Molecules, 2022, Vol 27, Issue 18, p6012
- ISSN
1420-3049
- Publication type
Article
- DOI
10.3390/molecules27186012