Diabetes Mellitus is a chronic disease in which the infected cells do not have the ability to produce sufficient amount of insulin that resulted in the abnormality of carbohydrates metabolism and an increase in blood glucose level. Long time exposure to Diabetes Mellitus resulted in failure or dysfunction of different organs like kidneys, nerves, heart, eyes, etc. A common practice to cure diabetes is the use of α-glucosidase inhibitors which help in lowering the blood glucose level. We presented 1,2-benzothiazine 1,1-dioxide derivatives as novel and more potent α-glucosidase inhibitors via their in vitro and in silico screenings. Excellent enzyme inhibitions were observed for compounds 2, 8, 10 and 12 having IC50 values of 6.91, 14.0, 4.2, 5.9 and 29.2μ respectively which were found better than the reference acarbose (IC50=38.31μM). Molecular docking studies suggested high binding energies and good binding interactions of these compounds with the active site residues of the receptor protein. A good agreement was found between the results of both modes of evaluation. Moreover, the envisioned candidates have a good potential to treat diabetes.

译文

:Diabetes Mellitus是一种慢性疾病,其中被感染的细胞无法产生足够量的胰岛素,从而导致碳水化合物代谢异常和血糖水平升高。长时间暴露于糖尿病会导致诸如肾脏,神经,心脏,眼睛等不同器官的衰竭或功能障碍。治疗糖尿病的一种常见做法是使用α-葡萄糖苷酶抑制剂来帮助降低血糖水平。通过体外和计算机筛选,我们提出了1,2-苯并噻嗪1,1-二氧化物衍生物,它们是新型且更有效的α-葡萄糖苷酶抑制剂。化合物2、8、10和12的IC50值分别为6.91、14.0、4.2、5.9和29.2μ,表现出优异的酶抑制作用,发现其优于参考阿卡波糖(IC50 =38.31μM)。分子对接研究表明这些化合物与受体蛋白的活性位点残基具有很高的结合能和良好的结合相互作用。在两种评估模式的结果之间都找到了很好的共识。此外,预想的候选人具有治疗糖尿病的良好潜力。

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