Anti-TMV activity based flavonol derivatives containing piperazine sulfonyl: Design, synthesis and mechanism study.

IF 3.9 2区化学 Q2 CHEMISTRY, APPLIED Molecular Diversity Pub Date : 2025-01-22 DOI:10.1007/s11030-025-11109-6

Zhiling Sun, Wei Zeng, Yujiao Qiu, Yuzhi Hu, Qing Zhou, Chunmei Hu, Yuhong Wang, Wei Xue

引用次数: 0

Abstract

A series of flavonoid derivatives containing piperazine sulfonate were designed and synthesized. The results of antiviral experiments in vivo showed that some target compounds had good inhibitory effect on tobacco mosaic virus (TMV). The EC₅₀ values of S15 and S19 curative activity were 174.5 and 110.4 μg/mL, respectively, which were better than 253.7 μg/mL of Ningnanmycin (NNM). The EC₅₀ values of S4 and S19 protection activity were 140.3 and 116.1 μg/mL, respectively, better than that of NNM (247.1 μg/mL). Microscale thermophoresis (MST) and molecular docking experiments showed that S19 had a good molecular binding force with TMV. Transmission electron microscopy (TEM) results show that S19 can fracture TMV particles and affect self-assembly. S19 treatment had almost no effect on the growth of seeds and seedlings, and can change the content of chlorophyll malondialdehyde (MDA) and superoxide dismutase (SOD) in tobacco to a certain extent, and improve the disease resistance of tobacco.

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基于抗tmv活性的哌嗪磺酰类黄酮醇衍生物的设计、合成及机理研究。

设计并合成了一系列含哌嗪磺酸盐的类黄酮衍生物。体内抗病毒实验结果表明，部分靶化合物对烟草花叶病毒（TMV）有较好的抑制作用。S15和S19的EC50值分别为174.5和110.4 μg/mL，优于宁南霉素（NNM）的253.7 μg/mL。S4和S19的EC50值分别为140.3和116.1 μg/mL，优于NNM （247.1 μg/mL）。微尺度热泳（MST）和分子对接实验表明，S19与TMV具有良好的分子结束力。透射电镜（TEM）结果表明，S19可以破坏TMV颗粒，影响其自组装。S19处理对种子和幼苗的生长几乎没有影响，但能在一定程度上改变烟草叶绿素丙二醛（MDA）和超氧化物歧化酶（SOD）的含量，提高烟草的抗病性。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Molecular Diversity 化学-化学综合

CiteScore

7.30

自引率

7.90%

发文量

219

审稿时长

2.7 months

期刊介绍： Molecular Diversity is a new publication forum for the rapid publication of refereed papers dedicated to describing the development, application and theory of molecular diversity and combinatorial chemistry in basic and applied research and drug discovery. The journal publishes both short and full papers, perspectives, news and reviews dealing with all aspects of the generation of molecular diversity, application of diversity for screening against alternative targets of all types (biological, biophysical, technological), analysis of results obtained and their application in various scientific disciplines/approaches including: combinatorial chemistry and parallel synthesis; small molecule libraries; microwave synthesis; flow synthesis; fluorous synthesis; diversity oriented synthesis (DOS); nanoreactors; click chemistry; multiplex technologies; fragment- and ligand-based design; structure/function/SAR; computational chemistry and molecular design; chemoinformatics; screening techniques and screening interfaces; analytical and purification methods; robotics, automation and miniaturization; targeted libraries; display libraries; peptides and peptoids; proteins; oligonucleotides; carbohydrates; natural diversity; new methods of library formulation and deconvolution; directed evolution, origin of life and recombination; search techniques, landscapes, random chemistry and more;