Synthesis and kinetics studies of N'-(2-(3,5-disubstituted-4H-1,2,4-triazol-4-yl)acetyl)-6/7/8-substituted-2-oxo-2H-chromen-3-carbohydrazide derivatives as potent antidiabetic agents.
A novel series of N'-(2-(3,5-disubstituted-4H-1,2,4-triazol-4-yl)acetyl)-6/7/8-substituted-2-oxo-2H-chromen-3-carbohydrazides were synthesized and studied for their α-glucosidase inhibition activity. Most of the synthesized compounds exhibited potential α-glucosidase inhibition activity with IC50 values ranging from 0.96 ± 0.02 to 32.86 ± 0.73 µg/ml. Among them, compounds 3e and 4e, having a methoxy group on the coumarin ring, proved to be the most potent ones, showing an enzyme inhibition activity with IC50  = 0.96 ± 0.02 and 1.44 ± 0.06 µg/ml, respectively. The kinetic study through Lineweaver-Burk plots revealed that the inhibition mechanism of the most active compounds 3d, 3e, 4d, and 4e, on the α-glucosidase activity, was found to be in the competitive mode.
['Menteşe|Emre|E|http://orcid.org/0000-0003-4105-8666', 'Baltaş|Nimet|N|http://orcid.org/0000-0003-4748-0665', 'Bekircan|Olcay|O|http://orcid.org/0000-0002-9609-8959']
D003374:Coumarins D015195:Drug Design D065089:Glycoside Hydrolase Inhibitors D006834:Hydrazines D020128:Inhibitory Concentration 50 D007700:Kinetics D015394:Molecular Structure D012441:Saccharomyces cerevisiae D013844:Thiazoles D000520:alpha-Glucosidases
kinetic study α-glucosidase inhibition coumarin 1,2,4-triazole