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合成 4-甲氧基苯甲酰腙并评价其抗糖基化活性。

Synthesis of 4-methoxybenzoylhydrazones and evaluation of their antiglycation activity.

机构信息

Atta-ur-Rahman Institute for Natural Product Discovery, Universiti Teknologi MARA, Puncak Alam Campus, Shah Alam 42300, Malaysia.

Research Institute of Chemistry, International Center for Chemical and Biological Sciences, University of Karachi, Karachi 75270, Pakistan.

出版信息

Molecules. 2014 Jan 21;19(1):1286-301. doi: 10.3390/molecules19011286.

Abstract

A series of 4-methoxybenzoylhydrazones 1-30 was synthesized and the structures of the synthetic derivatives elucidated by spectroscopic methods. The compounds showed a varying degree of antiglycation activity, with IC50 values ranging between 216.52 and 748.71 µM, when compared to a rutin standard (IC50=294.46±1.50 µM). Compounds 1 (IC50=216.52±4.2 µM), 3 (IC50=289.58±2.64 µM), 6 (IC50=227.75±0.53 µM), 7 (IC50=242.53±6.1) and 11 (IC50=287.79±1.59) all showed more activity that the standard, and these compounds have the potential to serve as possible leads for drugs to inhibit protein glycation in diabetic patients. A preliminary SAR study was performed.

摘要

合成了一系列 4-甲氧基苯甲酰腙 1-30,并通过光谱方法阐明了合成衍生物的结构。与芦丁标准品(IC50=294.46±1.50 μM)相比,这些化合物表现出不同程度的抗糖化活性,IC50 值在 216.52 至 748.71 μM 之间。化合物 1(IC50=216.52±4.2 μM)、3(IC50=289.58±2.64 μM)、6(IC50=227.75±0.53 μM)、7(IC50=242.53±6.1)和 11(IC50=287.79±1.59)均显示出比标准品更高的活性,这些化合物有可能成为抑制糖尿病患者蛋白质糖化的药物的潜在先导化合物。进行了初步的 SAR 研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/bf60/6271482/fe875a1ef20d/molecules-19-01286-g002.jpg

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