Abstract:
a-Glucosidase is a catabolic enzyme that regulates the body's plasma glucose levels by providing energy sources to maintain healthy functioning. 2-Amino-thiadiazole (1-13) and 2-amino-thiadiazole based Schiff bases (1422) were synthesized, characterized by 1 H NMR and HREI-MS and screened for a a-glucosidase inhibitory activity. All twenty-two (22) analogs exhibit varied degree of a-glucosidase inhibitory potential with IC50 values ranging between 2.30 ± 0.1 to 38.30 ± 0.7 µM, when compare with standard drug acarbose having IC50 value of 39.60 ± 0.70 µM. Among the series eight derivatives 1, 2, 6, 7, 14, 17, 19 and 20 showed outstanding a-glucosidase inhibitory potential with IC50 values of 3.30 ± 0.1, 5.80 ± 0.2, 2.30 ± 0.1, 2.70 ± 0.1, 2.30 ± 0.1, 5.50 ± 0.1, 4.70 ± 0.2, and 5.50 ± 0.2 µM respectively, which is many folds better than the standard drug acarbose. The remaining analogs showed good to excellent a-glucosidase inhibition. Structure activity relationship has been established for all compounds. The binding interactions of these compounds were confirmed through molecular docking.
Page(s):
0-0
DOI:
DOI not available
Published:
Journal: First International Conference on Revamped Scientific Outlook of 21st Century (Abstract Book), Volume: 0, Issue: 0, Year: 2022
Keywords:
molecular docking
,
Biological application
,
Onepot synthesis
,
Bisimidazole