Chemistry is the experimental and theoretical study of materials on their properties at both the macroscopic and microscopic levels. 102625-64-9, Name is 5-(Difluoromethoxy)-2-(((3,4-dimethoxypyridin-2-yl)methyl)thio)-1H-benzo[d]imidazole, molecular formula is C16H15F2N3O3S. In an article, author is Tafesse, Tadesse Bekele,once mentioned of 102625-64-9, Recommanded Product: 5-(Difluoromethoxy)-2-(((3,4-dimethoxypyridin-2-yl)methyl)thio)-1H-benzo[d]imidazole.
Synthesis and biological evaluation of 2-(2-methyl-1H-pyrrol-3-yl)-2-oxo-N-(pyridine-3-yl) acetamide derivatives: in vitro alpha-glucosidase inhibition, and kinetic and molecular docking study
One of the therapeutic approaches in the management of type 2 diabetes is delaying the glucose absorption through alpha-glucosidase enzyme inhibition, which can reduce the occurrence of postprandial hyperglycemia. Based on this thought, a series of novel chloro-substituted 2-(2-methyl-1-phenyl-1H-pyrrol-3-yl)-2-oxo-N-(pyridin-3-yl) acetamide derivatives 5a-i were synthesized and their alpha-glucosidase inhibitory activities were evaluated. All the synthesized compounds have shown moderate to excellent in vitro alpha-glucosidase inhibitory activity with IC50 values in the range of 111-673 mu M) as compared to acarbose, the standard drug (750 +/- 9 mu M). Compound 5e (111 +/- 12 mu M), among the series, was the most potent inhibitor of alpha-glucosidase in a competitive mode of action based on the kinetic study. The molecular docking study of compounds 5e and 5a revealed that they have a lower free binding energy (- 4.27 kcal/mol and – 3.17 kcal/mol, respectively) than acarbose (- 2.47 kcal/mol), which indicates that the target compound binds more easily to the enzyme than acarbose does. The outcomes from the molecular docking studies supported the results obtained from the in vitro assay. In conclusion, the overall results of our study reveal that the synthesized compounds could be a potential candidate in the search for novel alpha-glucosidase inhibitors to manage postprandial hyperglycemia incidence.
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Reference:
Pyridine – Wikipedia,
,Pyridine | C5H5N – PubChem