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噻唑衍生物作为新型α-葡萄糖苷酶抑制剂的合成、体外评价及分子对接研究

Synthesis, in vitro evaluation and molecular docking studies of thiazole derivatives as new inhibitors of α-glucosidase.

作者信息

Rahim Fazal, Ullah Hayat, Javid Muhammad Tariq, Wadood Abdul, Taha Muhammad, Ashraf Muhammad, Shaukat Ayesha, Junaid Muhammad, Hussain Shafqat, Rehman Wajid, Mehmood Rashad, Sajid Muhammad, Khan Muhammad Naseem, Khan Khalid Mohammed

机构信息

Department of Chemistry, Hazara University, Mansehra 21120, Pakistan.

Department of Chemistry, Hazara University, Mansehra 21120, Pakistan.

出版信息

Bioorg Chem. 2015 Oct;62:15-21. doi: 10.1016/j.bioorg.2015.06.006. Epub 2015 Jun 29.

Abstract

A series of thiazole derivatives 1-21 were prepared, characterized by EI-MS and (1)H NMR and evaluated for α-glucosidase inhibitory potential. All twenty one derivatives showed good α-glucosidase inhibitory activity with IC50 value ranging between 18.23±0.03 and 424.41±0.94μM when compared with the standard acarbose (IC50, 38.25±0.12μM). Compound (8) (IC50, 18.23±0.03μM) and compound (7) (IC50=36.75±0.05μM) exhibited outstanding inhibitory potential much better than the standard acarbose (IC50, 38.25±0.12μM). All other analogs also showed good to moderate enzyme inhibition. Molecular docking studies were carried out in order to find the binding affinity of thiazole derivatives with enzyme. Studies showed these thiazole analogs as a new class of α-glucosidase inhibitors.

摘要

制备了一系列噻唑衍生物1 - 21,通过电子轰击质谱(EI - MS)和氢核磁共振(¹H NMR)对其进行表征,并评估了它们对α - 葡萄糖苷酶的抑制潜力。与标准阿卡波糖(IC50,38.25±0.12μM)相比,所有二十一种衍生物均表现出良好的α - 葡萄糖苷酶抑制活性,IC50值在18.23±0.03至424.41±0.94μM之间。化合物(8)(IC50,18.23±0.03μM)和化合物(7)(IC50 = 36.75±0.05μM)表现出优异的抑制潜力,比标准阿卡波糖(IC50,38.25±0.12μM)要好得多。所有其他类似物也表现出良好到中等程度的酶抑制作用。进行了分子对接研究以确定噻唑衍生物与酶的结合亲和力。研究表明这些噻唑类似物是一类新型的α - 葡萄糖苷酶抑制剂。

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