In this study we are going to present thiazole based carbohydrazide in search of potent antidiabetic agent as α-amylase inhibitors. Thiazole based carbohydrazide derivatives 1-25 have been synthesized, characterized by 1HNMR, 13CNMR, and EI-MS, and evaluated for α-amylase inhibition. Except compound 11 all analogs showed α-amylase inhibitory activity with IC50 values from 1.709 ± 0.12 to 3.049 ± 0.25 μM against the standard acarbose (IC50 = 1.637 ± 0.153 μM). Compounds 1, 10, 14, and 20 exhibited outstanding inhibitory potential with IC50 value 1.763 ± 0.03, 1.747 ± 0.20, 1.709 ± 0.12, and 1.948 ± 0.23 μM, respectively, compared with the standard acarbose. Structure activity relationships have been established for the active compounds. To get an idea about the binding interaction of the compounds, molecular docking studies were done.

中文翻译：

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作为α-淀粉酶抑制剂的噻唑基碳酰肼衍生物及其分子对接研究

在这项研究中，我们将介绍基于噻唑的碳酰肼，以寻找有效的抗糖尿病药物作为 α-淀粉酶抑制剂。已合成基于噻唑的碳酰肼衍生物 1-25，通过 1HNMR、13CNMR 和 EI-MS 对其进行表征，并评估其对 α-淀粉酶的抑制作用。除化合物 11 外，所有类似物均显示出 α-淀粉酶抑制活性，对标准阿卡波糖的 IC50 值为 1.709 ± 0.12 至 3.049 ± 0.25 μM（IC50 = 1.637 ± 0.153 μM）。与标准阿卡波糖相比，化合物 1、10、14 和 20 表现出出色的抑制潜力，IC50 值分别为 1.763 ± 0.03、1.747 ± 0.20、1.709 ± 0.12 和 1.948 ± 0.23 μM。已建立活性化合物的构效关系。为了了解化合物的结合相互作用，进行了分子对接研究。