Fabrication of Furan-Functionalized Quinazoline Hybrids: Their Antibacterial Evaluation, Quantitative Proteomics, and Induced Phytopathogen Morphological Variation Studies,Journal of Agricultural and Food Chemistry

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Fabrication of Furan-Functionalized Quinazoline Hybrids: Their Antibacterial Evaluation, Quantitative Proteomics, and Induced Phytopathogen Morphological Variation Studies
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2019-09-26 , DOI: 10.1021/acs.jafc.9b03419
Qing-Su Long ₁ , Li-Wei Liu ₁ , Yong-Liang Zhao ₁ , Pei-Yi Wang ₁ , Biao Chen ₁ , Zhong Li ₂ , Song Yang _{1,

2}

Affiliation

The limited number of agrochemicals targeting plant bacterial diseases has driven us to develop highly efficient, low-cost, and versatile antibacterial alternatives. Herein, a novel type of simple furan-functionalized quinazolin-4-amines was systematically fabricated and screened for their antibacterial activity. Bioassay results revealed that compounds C₁ and E₄ could substantially block the growth of two frequently mentioned pathogens Xanthomonas oryzae pv oryzae and X. axonopodis pv citri in vitro, displaying appreciable EC₅₀ values of 7.13 and 10.3 mg/L, respectively. This effect was prominently improved by comparing those of mainly used agrochemicals. An in vivo experiment against bacterial blight further illustrated their viable applications as antimicrobial ingredients. Quantitative proteomics demonstrated that C₁ possessed a remarkable ability to manipulate the upregulation and downregulation of expressed proteins, which probably involved d-glucose and biotin metabolic pathways. This finding was substantially verified by parallel reaction monitoring analysis. Scanning electron microscopy images and fluorescence spectra also indicated that the designed compounds had versatile capacities for destroying the integrity of bacteria. Given these remarkable characteristics, furan-functionalized quinazoline hybrids can serve as a viable platform for developing innovative antibiotic alternatives against bacterial infections.

中文翻译：

呋喃功能化喹唑啉杂种的制备：抗菌评估，蛋白质组学和诱导的植物病原体形态变异研究。

针对植物细菌疾病的农用化学品数量有限，这驱使我们开发出高效，低成本和多功能的抗菌替代品。本文中，系统地制备了新型的简单呋喃官能化的喹唑啉-4-胺，并对其抗菌活性进行了筛选。生物测定结果表明，化合物c ^ ₁和Ë ₄能基本上阻挡两种经常提到的病原体的生长黄单胞菌PV菌和X. axonopodis PV柑橘体外，显示明显的EC ₅₀值分别为7.13和10.3 mg / L。通过比较主要使用的农用化学品的效果，该效果得到了显着改善。一项针对细菌性枯萎病的体内实验进一步说明了它们作为抗菌成分的可行性应用。定量蛋白质组学证明Ç ₁拥有操纵表达的蛋白质，这可能涉及到的上调和下调了非凡的能力d-葡萄糖和生物素代谢途径。通过平行反应监测分析基本上证实了这一发现。扫描电子显微镜图像和荧光光谱还表明，所设计的化合物具有破坏细菌完整性的多功能能力。鉴于这些显着的特征，呋喃官能化的喹唑啉杂种可以作为开发创新的抗生素替代物来抵抗细菌感染的可行平台。

更新日期：2019-09-26

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