State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Huaxi District, Guiyang 550025, China.
Division of Chemistry & Biological Chemistry, School of Physical & Mathematical Sciences, Nanyang Technological University, Singapore 637371, Singapore.
J Agric Food Chem. 2022 May 25;70(20):6050-6058. doi: 10.1021/acs.jafc.2c01407. Epub 2022 May 11.
A new class of axially chiral thiazine molecules were constructed and showed promising antibacterial activities against the plant pathogen pv. (). The axial chiralities of these compounds (- or -atropisomer) showed clear impacts on the in vitro inhibitory activities against . An optimal molecule of this class with the ()-axially chiral configuration was identified to exhibit inhibitory activity against with an EC value of 4.18 μg/mL. This inhibition efficiency is superior to that of two commercial antibacterial agrochemicals, thiodiazole-copper and bismerthiazol, as the positive controls. This hit compound also performed better than the controls in our in vivo studies. Preliminary mechanistic studies via scanning electron microscopy images showed that our hit compound at a concentration of 10 μg/mL destroyed the bacterial integrity of . Label-free quantitative proteomics analysis indicated that a total of 366 differentially expressed proteins of the rice plants were significantly influenced in the presence of our hit molecule.
一类新型的轴手性噻嗪分子被构建出来，并表现出对植物病原菌 pv. （）具有有前景的抗菌活性。这些化合物的轴手性（-或-对映异构体）对体外抑制活性对有明显影响。该类化合物中具有（）-轴手性构型的最佳分子被鉴定为对具有抑制活性，EC 值为 4.18 μg/mL。这种抑制效率优于作为阳性对照的两种商业抗菌农用化学品，噻二唑铜和双甲脒。该命中化合物在我们的体内研究中也表现优于对照。通过扫描电子显微镜图像进行的初步机制研究表明，我们的命中化合物在 10 μg/mL 的浓度下破坏了的细菌完整性。无标记定量蛋白质组学分析表明，在存在我们的命中分子的情况下，水稻植株中共有 366 种差异表达蛋白受到显著影响。
