含二苯醚部分的噻唑胺衍生物:设计、合成、杀真菌活性及对接研究

IF 1.7 4区 化学 Q3 Chemistry
Zhongzhong Yan, Yusheng Gao, Ziyu Yang, Bolin Yu, Di Zhao, Yuefeng Li, Lei Cao, Mengyao Qin, Mengmeng Li, Feng Jin
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引用次数: 0

摘要

设计、合成了几种含二苯基醚的噻唑胺衍生物,并对其抗真菌活性和细胞毒性进行了研究。其中,有几个化合物ⅱ对茄枯丝核菌具有较好的抑制作用,其抑制作用优于boscalid,与硫氟唑胺相当。此外,细胞毒性试验表明,最佳化合物IIf的细胞毒性总体上低于氟唑胺。此外,分子对接可以合理解释目标化合物的高活性。上述结果表明,含二苯醚部分的噻唑胺衍生物具有深入研究高效低毒绿色农药的价值。设计并合成了一系列新的含二苯基醚的噻唑胺衍生物。生物学评价表明,最佳化合物IIf不仅具有较高的杀真菌活性,而且具有较低的细胞毒性。此外,分子对接也为靶化合物的高活性提供了合理的解释。
本文章由计算机程序翻译,如有差异,请以英文原文为准。

Thiazolamide derivatives containing diphenyl ethers moiety: design, synthesis, fungicidal activity and docking study

Thiazolamide derivatives containing diphenyl ethers moiety: design, synthesis, fungicidal activity and docking study

Some thiazolamide derivatives containing diphenyl ether moiety were designed, synthesized, and studied for their antifungal activity and cell cytotoxicity. Of these, several compounds II possessed excellent activity against Rhizoctonia solani, which was better than that of boscalid and comparable to thifluzamide. Besides, the cytotoxicity test showed that the optimal compound IIf had lower cytotoxicity than thifluzamide in general. Further, molecular docking could give a reasonable explanation for the high activity of the target compounds. The above results indicated that thiazolamide derivatives containing diphenyl ether moiety are valuable for in-depth study to obtain high-efficiency and low-toxicity green pesticides.

Graphical abstract

A series of new thiazolamide derivatives containing diphenyl ether moiety were designed and synthesized. The biological evaluation indicated optimal compound IIf displayed not only high fungicidal activity but also lower cytotoxicity. Besides, molecular docking gave a reasonable explanation for the high activity of the target compounds.

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来源期刊
Journal of Chemical Sciences
Journal of Chemical Sciences Chemistry-General Chemistry
CiteScore
2.90
自引率
5.90%
发文量
107
审稿时长
12 months
期刊介绍: Journal of Chemical Sciences is a monthly journal published by the Indian Academy of Sciences. It formed part of the original Proceedings of the Indian Academy of Sciences – Part A, started by the Nobel Laureate Prof C V Raman in 1934, that was split in 1978 into three separate journals. It was renamed as Journal of Chemical Sciences in 2004. The journal publishes original research articles and rapid communications, covering all areas of chemical sciences. A significant feature of the journal is its special issues, brought out from time to time, devoted to conference symposia/proceedings in frontier areas of the subject, held not only in India but also in other countries.
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