Type-2 Diabetes Mellitus (T2DM) is one of the most common metabolic disorders in the world and over the past three decades its incidence has increased drastically. α-Glucosidase inhibitors are used to control the hyperglycemic affect of T2DM. Herein, we report the synthesis, α-glucosidase inhibition, structure activity relationship, pharmacokinetics and docking analysis of various novel chromone based thiosemicarbazones 3(a-r). The derivatives displayed potent activity against α-glucosidase with IC₅₀ in range of 0.11 ± 0.01–79.37 ± 0.71 µM. Among all the synthesized compounds, 3a (IC₅₀ = 0.17 ± 0.026 µM), 3 g (IC₅₀ = 0.11 ± 0.01 µM), 3n (IC₅₀ = 0.55 ± 0.02 µM), and 3p (IC₅₀ = 0.43 ± 0.025 µM) displayed higher inhibitory activity as compared to the standard, acarbose. Moreover, we have developed a statistically significant 2D-QSAR model (R²_tr:0.9693; F: 50.4647 and Q²_LOO:0.9190), which can be used in future to further design potent thiosemicarbazones as inhibitors of α-glucosidase.

2 型糖尿病 (T2DM) 是世界上最常见的代谢性疾病之一，在过去三十年中，其发病率急剧增加。α-葡萄糖苷酶抑制剂用于控制 T2DM 的高血糖影响。在此，我们报道了各种新型色酮基缩氨基硫脲3(ar)的合成、α-葡萄糖苷酶抑制、结构活性关系、药代动力学和对接分析。这些衍生物对α-葡萄糖苷酶表现出有效的活性，IC ₅₀范围为 0.11 ± 0.01–79.37 ± 0.71 µM。在所有合成的化合物中，3a ( IC ₅₀  = 0.17 ± 0.026 µM)、3 g (IC ₅₀  = 0.11 ± 0.01 µM)、3n ( IC ₅₀  = 0.55 ± 0.02 µM) 和3p ( IC ₅₀  = 0.43 ± 0.025 µM) ）与标准阿卡波糖相比显示出更高的抑制活性。此外，我们还开发了具有统计显着性的2D-QSAR模型（​​R ² _tr：0.9693；F：50.4647和Q ² _LOO：0.9190），该模型将来可用于进一步设计有效的缩氨基硫脲作为α-葡萄糖苷酶抑制剂。