Synthesis of diethyl 4-substituted-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylates as a new series of inhibitors against yeast α-glucosidase

Synthesis, Biological Evaluation and Molecular Docking Study of 2-Substituted-4,6-Diarylpyrimidines as α-Glucosidase Inhibitors

“…Results are summarized in Table 1 . The majority of the screened compounds possessed significant α-glucosidase inhibitory activity, with IC 50 values ranging from 19.6 ± 0.21 to 38.9 ± 0.35 μM, more potent than the positive control α-glucosidase inhibitor acarbose (IC 50 = 817.38 ± 6.27 μM, the value of IC 50 was similar to that reported previously in the literature [ 23 , 24 ]), which is currently clinically used as an anti-diabetic agent to control blood glucose level of patients. Compounds 6a , 6b , 6d , 6j , 6k , 6s and 6t displayed potent inhibitory activities, with IC 50 values of 20.4 ± 0.23, 23.7 ± 0.27, 29.0 ± 0.28, 19.6 ± 0.21, 21.2 ± 0.25, 26.2 ± 0.27 and 25.3 ± 0.28 μM, respectively.…”

Synthesis and Cytotoxicity of 1,4‐Dihydropyridines and an Unexpected 1,3‐Oxazin‐6‐one

“…The structures of 6 – 9 and 11 were previously reported , while 5 , 10 , and 12 are reported for the first time.…”

Synthesis, Biological Evaluation, and Molecular Docking Studies of Novel Isatin-Thiazole Derivatives as α-Glucosidase Inhibitors

“…All the synthetic compounds 6a – 6p were screened for their in vitro α-glucosidase inhibitory activity ( Table 1 ). The results were shown that all the tested compounds displayed potent to moderate α-glucosidase inhibitory activity with IC 50 ranging from 5.36 ± 0.13 to 35.76 ± 0.31 μm more potent than the standard drug acarbose (IC 50 = 817.38 ± 6.27 μm [ 17 , 36 ]). Among the series, compounds 6a , 6g , 6h , 6i , 6j , 6l , 6m , 6n , and 6p displayed potent inhibitory activity with IC 50 values of 6.87 ± 0.14, 5.98 ± 0.12, 6.12 ± 0.15, 7.51 ± 0.17, 6.51 ± 0.13, 8.33 ± 0.18, 7.17 ± 0.15, 6.36 ± 0.12, and 5.36 ± 0.13 μm.…”

“…According to the literature procedure [ 36 ], α-Glucosidase inhibitory activity was assayed by using 0.1 M phosphate buffer (pH 6.8) at 37 °C. The enzyme (0.1 U/mL) in phosphate buffer saline was incubated with various concentrations of test compounds at 37 °C for 15 min.…”