A new series of thiobarbituric (thiopyrimidine trione) enamine derivatives and its analogues barbituric acid derivatives was synthesised, characterised, and screen for in vitro evaluation of α-glucosidase enzyme inhibition and anti-glycation activity. This series of compounds were found to inhibit α-glucosidase activity in a reversible mixed-type manner with IC50 between 264.07 ± 1.87 and 448.63 ± 2.46 µM. Molecular docking studies indicated that compounds of 3g, 3i, 3j, and 5 are located close to the active site of α-glucosidase, which may cover the active pocket, thereby inhibiting the binding of the substrate to the enzyme. Thiopyrimidine trione derivatives also inhibited the generation of advanced glycation end-products (AGEs), which cause long-term complications in diabetes. While, compounds 3a-k, 5, and 6 showed significant to moderate anti-glycation activity (IC50 = 31.5 ± 0.81 to 554.76 ± 9.1 µM).

中文翻译：

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硫代巴比妥酸烯胺衍生物的合成与表征，及其α-葡萄糖苷酶抑制和抗糖基化活性的评估。

合成，表征和表征了一系列新的硫代巴比妥酸（硫代嘧啶三酮）烯胺衍生物及其类似物巴比妥酸衍生物，用于体外评估α-葡萄糖苷酶的抑制作用和抗糖化活性。发现该系列化合物以可逆的混合型方式抑制α-葡萄糖苷酶活性，IC50在264.07±1.87和448.63±2.46 µM之间。分子对接研究表明3g，3i，3j和5的化合物位于α-葡萄糖苷酶的活性位点附近，该活性位点可能覆盖了活性囊，从而抑制了底物与酶的结合。硫嘧啶三酮衍生物还抑制晚期糖基化终产物（AGEs）的产生，后者会导致糖尿病的长期并发症。而化合物3a-k，5