Synthesis and Biological Activity of Chalcone Derivatives Containing Thiazoxime Ethers

文献类型： 外文期刊

第一作者： Qin, Yishan

作者： Qin, Yishan;Sun, Nan;Li, Jieyu;Yang, Han;Pu, Haotao;Wang, Yuhong;Luo, Xingping;Xue, Wei;Qin, Yishan;Zhang, Jing

作者机构：

期刊名称：JOURNAL OF HETEROCYCLIC CHEMISTRY （ 影响因子：2.4； 五年影响因子：2.2 ）

ISSN： 0022-152X

年卷期： 2025 年

页码：

收录情况： SCI

摘要： In this paper, a series of chalcone derivatives containing thiazole oxime ether structures were designed and synthesized from the natural product chalcone. The structures of these compounds were characterized using nuclear magnetic resonance (NMR) and high-resolution mass spectrometry (HRMS). The results of antiviral activity tests showed that some of the target compounds exhibited better inhibition. Among them, S3, S4, and S16 exhibited better therapeutic activities with EC50 values of 18.6, 66.9, and 61.8 mu g/mL, respectively, which were superior to that of the control drug ningnanmycin (158.3 mu g/mL). The target compound S3 showed good protective activity with an EC50 of 88.6 mu g/mL, which was better than that of ningnanmycin (175.6 mu g/mL). The results of microscale thermophoresis (MST) demonstrated that S3 and S13 exhibited strong binding affinity to tobacco mosaic virus capsid protein (TMV-CP), with Kd values of 0.0013 mu M and 0.5397 mu M, respectively. These values were significantly lower than that of ningnanmycin (Kd = 0.6509 mu M). The molecular docking results showed that the hydrogen bonds between S3 and the key amino acid residues of TMV-CP had shorter bond lengths and were more tightly bound than those of ningnanmycin.

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