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新型含乙缩醛和嘧啶的磺胺类化合物的合成、抗菌活性及作用机制。

Synthesis, Antibacterial Activity, and Action Mechanism of Novel Sulfonamides Containing Oxyacetal and Pyrimidine.

机构信息

State Key Laboratory Breeding Base of Green Pesticide and Agricultural Bioengineering, Key Laboratory of Green Pesticide and Agricultural Bioengineering, Ministry of Education, Guizhou University, Guiyang 550025, P. R. China.

出版信息

J Agric Food Chem. 2022 Aug 3;70(30):9305-9318. doi: 10.1021/acs.jafc.2c02099. Epub 2022 Jul 20.

Abstract

Bacterial leaf blight (BLB) and bacterial leaf streak (BLS) are two serious bacterial diseases caused by pv. () and pv. (), respectively. However, the control of these diseases by conventional pesticides remains challenging due to development of resistances. We aimed to address this pending problem and developed a series of novel pyrimidine sulfonamide derivatives. Structurally, title compounds bear a unique oxyacetal group, which has a proven immune-activating effect. Compound designed based on the 3D-QSAR model was demonstrated as the optimal activity against and , with EC values of 26.7 and 30.8 mg/L, respectively, which were higher than the positive controls bismerthiazol (29.9 and 32.7 mg/L) and thiodiazole copper (30.5 and 36.4 mg/L). On the prevention level, the biological activity test showed compound had superior protective activity (43.7%) on BLS to thiodiazole copper (32.1%). The defense enzymes and proteomics results suggested that compound could be a versatile candidate as it improved plant's resistance to disease.

摘要

细菌性叶斑病 (BLB) 和细菌性条斑病 (BLS) 是由 pv. () 和 pv. () 分别引起的两种严重的细菌性疾病。然而,由于抗药性的发展,常规农药对这些疾病的控制仍然具有挑战性。我们旨在解决这一待解决的问题,并开发了一系列新型嘧啶磺酰胺衍生物。从结构上看,标题化合物具有独特的氧缩醛基团,已被证明具有免疫激活作用。根据 3D-QSAR 模型设计的化合物 对 和 表现出最佳的 活性,EC 值分别为 26.7 和 30.8 mg/L,高于阳性对照双脒噻唑 (29.9 和 32.7 mg/L) 和噻二唑铜 (30.5 和 36.4 mg/L)。在预防水平上,生物活性测试表明,化合物 对 BLS 的保护活性 (43.7%)优于噻二唑铜 (32.1%)。防御酶和蛋白质组学结果表明,化合物 可以作为一种多功能候选药物,因为它可以提高植物对疾病的抗性。

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