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肼基噻唑羧酸酯的合成:一种治疗糖尿病及其并发症的机制方法。

Synthesis of hydrazinylthiazole carboxylates: a mechanistic approach for treatment of diabetes and its complications.

机构信息

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.

出版信息

Future Med Chem. 2023 Jul;15(13):1149-1165. doi: 10.4155/fmc-2023-0136. Epub 2023 Aug 8.

Abstract

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.

摘要

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。

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