Chalcone derivatives containing 1,2,4-triazole and pyridine moiety: design, synthesis, and antiviral activity.

IF 3.9 2区化学 Q2 CHEMISTRY, APPLIED Molecular Diversity Pub Date : 2024-12-02 DOI:10.1007/s11030-024-11049-7

Hui Xin, Jiao Tian, Tianyu Deng, Qing Zhou, Yuhong Wang, Hong Fu, Haotao Pu, Wei Xue

引用次数: 0

Abstract

A series of chalcone derivatives containing 1,2,4-triazole and pyridine were designed and synthesized, and their antiviral activities against tobacco mosaic virus (TMV) were evaluated. Notably, S7 (EC₅₀ = 89.7 μg/mL) exhibited excellent curative activity against the TMV, which was superior to that of ningnanmycin (NNM: EC₅₀ = 201.7 μg/mL). Molecular docking showed that S7 exhibited satisfactory affinities for the TMV coat protein (TMV-CP), with four strong conventional hydrogen bonds with amino acid residues. Further, microscale thermophoresis (MST) showed that S7 (Kd = 0.5340 ± 0.2233 μmol/L) bound more strongly to TMV-CP than NNM (Kd = 5.1186 ± 1.9568 μmol/L). The results of chlorophyll content, malondialdehyde (MDA) content, and biological enzyme activity confirmed that S7 enhanced the disease resistance of tobacco plants by affecting the change of chlorophyll content, interfering with plant lipid peroxidation, and enhancing SOD activity in plants, respectively.

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含有1,2,4-三唑和吡啶的查尔酮衍生物：设计、合成和抗病毒活性。

设计合成了一系列含有1,2,4-三唑和吡啶的查尔酮衍生物，并对其抗烟草花叶病毒（TMV）的活性进行了评价。值得注意的是，S7 （EC50 = 89.7 μg/mL）对TMV表现出良好的治疗活性，优于宁南霉素（NNM: EC50 = 201.7 μg/mL）。分子对接表明，S7与TMV外壳蛋白（TMV- cp）具有良好的亲和性，与氨基酸残基形成4个强常规氢键。微尺度热电泳（MST）结果表明，S7 （Kd = 0.5340±0.2233 μmol/L）与TMV-CP的结合比NNM （Kd = 5.1186±1.9568 μmol/L）强。叶绿素含量、丙二醛（MDA）含量和生物酶活性的测定结果证实，S7分别通过影响叶绿素含量的变化、干扰植物脂质过氧化和提高植物SOD活性来增强烟草植株的抗病性。

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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SOD Activity enzyme assay reagent kits

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;