Synthesis, structure, and evaluation of in vitro α-glucosidase enzyme inhibition of a new class of diethylammonium salts of aryl substituted thiobarbituric acid is described. This protocol is straight, environmentally benign and efficient, involving Aldol-Michael addition reaction in one pot fashion. The 3D chemical structures of the synthesized compounds were assigned based on spectroscopic methods and X-ray single crystal diffraction analyses. All synthesized compounds 3a-3n were evaluated for their in vitro α-glucosidase enzyme inhibitory activity, whereas acarbose was used as the standard drug (IC₅₀ = 840 ± 1.73 µM). All tested compounds were found to possess varying degree of α-glucosidase enzyme inhibition activity with (IC₅₀ = 19.46 ± 1.84–415.8 ± 4.0 µM). Compound 3i (IC₅₀ = 19.4 ± 1.84 µM) exhibited the highest activity. To the best of knowledge this is the first report of the in vitro α-glucosidase enzyme inhibition by the diethylamonium salts of aryl substituted thiobarbituric acid. Furthermore, molecular docking studies of selected compounds were also performed to see interactions between active compounds and binding sites.

描述，体外α-葡萄糖苷酶抑制一类新的芳基取代的硫代巴比妥酸二乙铵盐的合成，结构和评价。该方案是直接的，对环境无害且有效的，涉及以一锅法进行的Aldol-Michael加成反应。基于光谱方法和X射线单晶衍射分析，确定了合成化合物的3D化学结构。所有合成的化合物3A - 3N它们进行了评价体外α葡萄糖苷酶抑制活性，而阿卡波糖用作标准药物（IC ₅₀  = 840±1.73μM）。发现所有测试的化合物均具有不同程度的α-葡糖苷酶的酶抑制活性为（IC ₅₀  = 19.46±1.84–415.8±4.0 µM）。化合物 3i  （IC ₅₀  = 19.4±1.84 µM）表现出最高的活性。就其所知，这是关于芳基取代的硫代巴比妥酸的二乙基铵盐抑制体外α-葡萄糖苷酶的报道。此外，还进行了所选化合物的分子对接研究，以观察活性化合物与结合位点之间的相互作用。