乌拉水子:设计,合成,抗微生物活性和假定作用方式
Huan Zhou1, Qing X Li2, Lei Zeng1
1Key Laboratory of Pesticide and Chemical Biology of Ministry of Education, College of Chemistry, Central China Normal University, Wuhan, China.
Pest management science
|September 14, 2023
概括
新型 uracil hydrazones 对植物病原体具有强烈的抗菌活性. 化合物IV-B20有效地对抗作物中的真菌和细菌疾病,为传统农药提供了一个有希望的替代品.
科学领域:
- 农业化学 农业化学
- 植物病理学 植物病理学
- 药用化学 医学化学
背景情况:
- 由真菌和细菌引起的作物疾病导致全球粮食生产的重大损失.
- 传统的化学农药面临着诸多挑战,包括微生物耐药性和环境污染.
- 开发新的,有效的杀菌剂和杀菌剂对于可持续农业至关重要.
研究的目的:
- 设计和评估新型 uracil 化衍生物对抗植物病原体的抗菌疗效.
- 识别有潜在应用在作物保护中的强效化合物.
- 研究最有效化合物的作用机制.
主要方法:
- 一系列 uracil 化衍生物 (IV-B) 的合成.
- 在体外生物测试以确定对真菌和细菌植物病原体的抑制率.
- 在体内有效性测试,将化合物与商业标准进行比较.
- 机理学研究以阐明作用模式.
主要成果:
- 大多数 uracil hydrazones (IV-B) 对Monilia fructigena,Sclerotium rolfsii,Clavibacter michiganensis亚种进行了80%以上的抑制. 密西班牙人,Xanthomonas oryzae pv. 在美国. 在实验室中,Oryzae和Ralstonia solanacearum.
- 化合物IV-B20在体内表现出优异的治疗 (89.9%) 和保护 (71.8%) 活性,对C. michiganensis亚种. 密歇根州与基于铜的杀菌剂相比.
- IV-B20对M. fructigena (96.3%) 和S. rolfsii (80.4%) 的保护活性非常出色,其性能优于或与现有的杀菌剂相匹配.
- 机理学研究表明,IV-B20会诱导致病性细菌的氧化损伤和细胞泄漏.
结论:
- 乌拉基衍生物IV-B20显示出作为农业应用的新型抗菌剂的巨大潜力.
- 这些发现为开发新的作物保护策略提供了基础.
- IV-B20的机制包括在细菌病原体中诱导氧化应激.
相关概念视频
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
3.0K
The reaction of weakly electrophilic aryldiazonium (also called arenediazonium) salts with highly activated aromatic compounds leads to the formation of products with an —N=N— link, called an azo linkage. This reaction, presented in Figure 1, is known as diazo coupling and occurs without the loss of the nitrogen atoms of the aryldiazonium salt. Highly activated aromatic compounds such as phenols or arylamines favor the diazo coupling reaction. The coupling generally occurs at the...
3.0K
Diazonium Group Substitution: –OH and –H
2.8K
Nitrous acid, a weak acid, is prepared in situ via the reaction of sodium nitrite with a strong acid under cold conditions. This nitrous acid prepared in situ reacts with primary arylamines to form arenediazonium salts. Such reactions are known as diazotization reactions. As shown in Figure 1, the formation of arenediazonium salts begins with the decomposition of nitrous acid in an acidic solution to give nitrosonium ions.
2.8K
Preparation of 1° Amines: Azide Synthesis
4.0K
Direct alkylation of ammonia produces polyalkylated amines, along with a quaternary ammonium salt. To exclusively prepare primary amines, the azide synthesis method can be used.
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
Azide ions act as good nucleophiles and react with unhindered alkyl halides to form alkyl azides. Alkyl azides do not participate in further nucleophilic substitution reactions, thereby eliminating the chances of polyalkylated products. Alkyl azides are reduced by hydride-based reducing agents, like lithium aluminum...
4.0K
Aldehydes and Ketones with HCN: Cyanohydrin Formation Overview
2.8K
Cyanohydrins are compounds that contain –CN and –OH groups on the same carbon atom. They are formed by the nucleophilic addition of the cyanide ions to the carbonyl group. Cyanide ions are highly basic and nucleophilic and can be generated from HCN under aqueous conditions. However, since HCN is a weak acid, the number of cyanide ions generated is very small. Hence, a small amount of base or KCN/NaCN is added to HCN to increase the concentration of the cyanide ions in the reaction...
2.8K
Aldehydes and Ketones with HCN: Cyanohydrin Formation Mechanism
3.2K
Cyanohydrins are formed when cyanide nucleophiles and carbonyl compounds like aldehydes and ketones react. A strong base, the cyanide ion, catalyzes cyanohydrin formation. The ions are generated from HCN under aqueous conditions. Once the cyanide ions are generated, the first step involves the nucleophilic attack of the cyanide ions on the electrophilic carbonyl carbon. This attack shifts the π electrons from the C=O to the oxygen atom forming the alkoxide ion intermediate. The alkoxide anion...
3.2K
Preparation of Amides
3.1K
Amides are synthesized by treating carboxylic acids with amines in the presence of dehydrating agents like dicyclohexylcarbodiimide (DCC).
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
The DCC-promoted synthesis of amides begins with the protonation of DCC by carboxylic acid. The protonation makes it a better acceptor. Next, the addition of carboxylate to the protonated carbodiimide gives a reactive acylating agent.
Subsequently, the amine acts as a nucleophile that attacks the acylating agent to form a tetrahedral intermediate. In the...
3.1K


