合成,纳米杀伤性评估,以及对奥龙衍生物的结构-活动关系研究
Xiaofeng Cao1, Mingxia Wang1, Zhong Li1
1Shanghai Key Laboratory of Chemical Biology, School of Pharmacy, East China University of Science and Technology, Shanghai 200237, China.
Journal of agricultural and food chemistry
|June 5, 2023
概括
新的奥龙类类似物显示出对植物寄生性线虫 (PPNs) 的强烈杀菌活性. 化合物32在体外和体内显著控制了Meloidogyne incognita,为农业害虫管理提供了一个有希望的途径.
科学领域:
- 农业科学 农业科学
- 有机化学 有机化学
- 遗体学 遗体学 是一个学科.
背景情况:
- 植物寄生性线虫 (PPNs) 对全球农业构成重大威胁.
- 有效的化学杀虫剂对于管理PPN至关重要.
- 欧龙类类似物因其潜在的杀菌性质而受到探索.
研究的目的:
- 合成和评估新型aurone类型对植物寄生性线虫的杀虫活性.
- 分析合成化合物的结构-活性关系.
- 为了有效地控制线虫,识别化合物.
主要方法:
- 使用混合3D相似性计算方法 (SHAFTS) 设计光环类相似物.
- 合成了37种光环类同类化合物.
- 评估了对Meloidogyne incognita (根结线虫) 和Caenorhabditis elegans的杀菌活性.
主要成果:
- 化合物6及其衍生品表现出显著的杀菌活性.
- 化合物32是一种6F替代的光类型,表现出最强烈的活性.
- 化合物32的LC50/72h为1.75mg/L对M.incognita,在沙子中抑制97.93%,并抑制了蛋和C.elegans的运动.
结论:
- 欧龙类类似物,特别是化合物32,是控制植物寄生性线虫的一类有前途的化合物.
- 鉴定到的结构-活动关系可以指导开发更有效的杀虫剂.
- 化合物32为可持续农业害虫管理提供了一个潜在的解决方案.
相关概念视频
Physical Properties of Amines
3.3K
Amines with low molecular weight are usually gaseous at room temperature, while those with high molecular weight are liquid or solids in nature. Usually, low molecular weight amines have a rotten fish-like smell. Diamines typically have a pungent smell. For instance, cadaverine and putrescine, depicted in Figure 1, are two molecules responsible for decaying tissue.
3.3K
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
Adrenergic Agonists: Chemistry and Structure-Activity Relationship
3.1K
Adrenergic agonists' structure-activity relationship (SAR) determines their selectivity and efficacy. These agonists comprise a phenylethylamine moiety with an aromatic ring and an ethylamine side chain.
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
Aromatic ring substitutions: Substituting the aromatic ring with –OH groups at positions 3 and 4 yields catecholamines (e.g., epinephrine), which have a high affinity for adrenoceptors. Hydrogen bonding between –OH groups and receptors enhances adrenergic activity.
Separation of...
3.1K
Local Anesthetics: Chemistry and Structure-Activity Relationship
4.5K
Local anesthetics (LAs) are drugs that induce a temporary loss of sensation in a limited body area, preventing pain. Cocaine was the first local anesthetic discovered in the late 19th century. Cocaine is a benzoic acid ester obtained from the leaves of coca shrubs and was often used for its psychotropic effects. Cocaine was first isolated in 1860 by Albert Niemann. Sigmund Freud studied the physiological actions of cocaine. Carl Koller later introduced it into clinical practice in 1884 as a...
4.5K
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
2.1K
Treating arylamines with nitrous acid gives aryldiazonium salts that are effective substrates in nucleophilic aromatic substitution reactions. The diazonio group in these salts can be easily displaced by different nucleophiles, yielding a wide variety of substituted benzenes. The leaving group departs as nitrogen gas, and this easy elimination is the driving force for the substitution reaction.
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...
2.1K
Basicity of Aromatic Amines
7.2K
The basicity of aromatic amines is much weaker than that of aliphatic amines due to the involvement of the lone pair of electrons over the N atom in resonance with the aryl rings. Generally, the electron-donating ability of any substituents on the aryl ring of aromatic amines increases the basicity of the amine by increasing electron density, and hence the availability of lone pair on the nitrogen. On the other hand, electron-withdrawing functional groups on the aryl ring of amines decrease the...
7.2K


