Department of Chemistry, Mirpur University of Science & Technology (MUST), Mirpur (AJK), 10250, Pakistan.
Department of Chemistry & Biochemistry, Miami University, 651 E. High Street, Oxford, OH 45056, USA.
Future Med Chem. 2023 Jul;15(13):1149-1165. doi: 10.4155/fmc-2023-0136. Epub 2023 Aug 8.
The deaths of thousands of people and millions affected by diabetes mellitus triggered us to look for alternative possible solutions to cure diabetes and its complications. A series of hydrazinylthiazole carboxylates () was prepared by cyclocondensation reaction of thiosemicarbazones with ethyl 2-chloroacetoacetate. These compounds were screened for antidiabetic potential through α-amylase inhibition, antiglycation and antioxidant assays. Most of the compounds exhibited a promising antidiabetic property. Compounds and showed excellent α-amylase and glycation inhibition properties. The hemolytic assay indicated that all compounds are biocompatible. Docking studies carried out on α-amylase target showed correlation between inhibition and binding energy.
成千上万的人因糖尿病死亡，数百万人受到影响，这促使我们寻找治疗糖尿病及其并发症的替代方法。通过缩硫酮与乙基 2-氯乙酰乙酸酯的环缩合反应，合成了一系列肼基噻唑羧酸酯（）。通过α-淀粉酶抑制、糖化抑制和抗氧化测定筛选这些化合物的抗糖尿病潜力。大多数化合物表现出有希望的抗糖尿病特性。化合物和表现出优异的α-淀粉酶和糖化抑制特性。溶血试验表明所有化合物均具有生物相容性。对α-淀粉酶靶标进行的对接研究表明，抑制作用与结合能之间存在相关性。
