2-氧代-N-苯基乙酰胺衍生物的合成及其抗菌活性,Journal of Agricultural and Food Chemistry

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2-氧代-N-苯基乙酰胺衍生物的合成及其抗菌活性
Journal of Agricultural and Food Chemistry ( IF 5.7 ) Pub Date : 2022-07-21 , DOI: 10.1021/acs.jafc.2c02605
Awei Zhang ₁ , Runjiang Song ₁ , Ronghua Wang ₁ , Hongde Li ₁ , Deyu Hu ₁ , Baoan Song ₁

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水稻白叶枯病和水稻白条病是两种严重的水稻病害，对世界范围内的水稻生产造成了极大的危害。为了开发具有新靶点的高效抗菌剂，合成了一系列含有二砜部分的新型2-氧代-N-苯乙酰胺衍生物，并对其抗菌活性进行了评价。其中，化合物D ₁₄表现出最好的抗菌活性，尤其是对Xoo和Xoc的抑菌活性， EC ₅₀值分别为0.63和0.79 mg/L，明显优于商业对照的双甲基噻唑（BT ）。)（分别为 76.59 和 83.35 mg/L）和噻二唑铜 ( TC )（分别为 91.72 和 114.00 mg/L）。同时，化合物D ₁₄^{可以与 Pxo99 A}的 CRP 样蛋白 (Clp) 相互作用，并与Xoo -Clp表现出强结合活性， K _d值为 0.52 μM，远优于BT的相应K _d值。 183.94 μM ) 和TC (222.58 μM)。D ₁₄的处理和clp基因的缺失可以显着降低clp的表达基因并减弱病原菌的毒力。这些结果表明化合物D ₁₄可作为一种潜在的新型农业杀菌剂，而Clp可作为控制植物细菌病害的靶蛋白。该工作为开发以Clp为靶蛋白的新型抗菌剂提供了可靠的支持。

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Synthesis and Antibacterial Activities of 2-Oxo-N-phenylacetamide Derivatives Containing a Dissulfone Moiety Target on Clp

Rice bacterial blight and rice bacterial streak are two serious rice diseases and have caused great harm to the production of rice all over the world. To develop an efficient antibacterial agent with a novel target, a series of novel 2-oxo-N-phenylacetamide derivatives containing a dissulfone moiety were synthesized, and their antibacterial activities were evaluated. Among them, compound D₁₄ exhibited the best antibacterial activities, especially against Xoo and Xoc with EC₅₀ values of 0.63 and 0.79 mg/L, respectively, which were much better than the commercial control of bismerthiazol (BT) (76.59 and 83.35 mg/L, respectively) and thiodiazole copper (TC) (91.72 and 114.00 mg/L, respectively). Meanwhile, compound D₁₄ can interact with a CRP-like protein (Clp) of Pxo99^A and show strong binding activity with Xoo-Clp with a K_d value of 0.52 μM, which was far superior to the corresponding K_d values of BT (183.94 μM) and TC (222.58 μM). Treatment of D₁₄ and deletion of the clp gene could significantly reduce the expression of the clp gene and attenuate the virulence of pathogenic bacteria. These results indicated that compound D₁₄ could be used as a potential novel agricultural bactericide and Clp can be used as a target protein for the control of plant bacterial diseases. This work provided reliable support for developing novel antibacterial agents based on Clp as a target protein.

更新日期：2022-07-21

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