α-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 (14–22) were synthesized, characterized by ¹H NMR and HREI-MS and screened for α-glucosidase inhibitory activity. All twenty-two (22) analogs exhibit varied degree of α-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 α-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 fold better than the standard drug acarbose. The remaining analogs showed good to excellent α-glucosidase inhibition. Structure activity relationship has been established for all compounds. The binding interactions of these compounds were confirmed through molecular docking.

α-葡萄糖苷酶是一种分解代谢酶，通过提供能量来维持健康功能来调节人体的血浆葡萄糖水平。2-氨基噻二唑（1 - 13）和2-氨基噻二唑基席夫碱（14 - 22）的合成，其特征在于，¹ H NMR和HREI-MS并筛选α葡萄糖苷酶抑制活性。与具有IC ₅₀值为39.60±0.70μM的标准阿卡波糖相比，所有二十二（22）个类似物均表现出不同程度的α-葡萄糖苷酶抑制潜力，IC ₅₀值为2.30±0.1至38.30± 0.7μM。间的系列8个衍生物1，2，6，7，14，17，19和20显示出杰出的α葡萄糖苷酶抑制潜力与IC _50倍的3.30±0.1的值，5.80±0.2，2.30±0.1，2.70±0.1，2.30±0.1，5.50±0.1，4.70分别为±0.2和5.50±0.2μM，比标准药物阿卡波糖好几倍。其余类似物表现出良好至优异的α-葡萄糖苷酶抑制作用。已经为所有化合物建立了结构活性关系。这些化合物的结合相互作用通过分子对接得以证实。