Abstract
Aimed at finding new compounds capable of inhibiting the enzyme glucosidase, six new N-(5-aryliden-4-oxo-2-thioxothiazolidin-3-yl)-2-{[4-oxo-3-(p-tolyl)-3,4-dihydro quinazolin-2-yl]thio}acetamides 5a-f were synthesized by the reaction of N-(4-oxo-2-thioxothiazolidin-3-yl)-2-{[4-oxo-3-(p-tolyl)-3,4-dihydroquinazolin-2-yl]thio}acetamide 4 and appropriate aromatic aldehydes. The structural features of all synthesized compounds were confirmed based on their spectral data, including HR-MS, IR, 1H-NMR and 13C-NMR spectra. The results of the evaluation of the α-glucosidase enzyme inhibitory activity of acetamide compounds 5a-f showed that these compounds possess good inhibitor activity against the α-glucosidase enzyme, in which compound 5a containing the 4-methylbenzylidene moiety exhibited the best activity. Furthermore, molecular docking was conducted to better comprehend the binding properties of the compounds. The results indicated that synthesized quinazoline derivatives are potential antidiabetic compounds.
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