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相关概念视频

ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH301:11

ortho–para-Directing Activators: –CH3, –OH, –⁠NH2, –OCH3

6.1K
All ortho–para directors, excluding halogens, are activating groups. These groups donate electrons to the ring, making the ring carbons electron-rich. Consequently, the reactivity of the aromatic ring towards electrophilic substitution increases. For instance, the nitration of anisole is about 10,000 times faster than the nitration of benzene. The electron-donating effect of the methoxy group in anisole activates the ortho and para positions on the ring and stabilizes the corresponding...
6.1K
Basicity of Heterocyclic Aromatic Amines01:25

Basicity of Heterocyclic Aromatic Amines

6.1K
Heterocyclic amines, where the N atom is a part of an alicyclic system, are similar in basicity to alkylamines. Interestingly, the heterocyclic amine having a nitrogen atom as part of an aromatic ring has much less basicity than its corresponding alicyclic counterpart. For this reason, as presented in Figure 1, piperidine (pKb = 2.8) is significantly more basic than pyridine (pKb = 8.8).
6.1K
Aryldiazonium Salts to Azo Dyes: Diazo Coupling01:11

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
Five-Membered Heterocyclic Aromatic Compounds: Overview01:13

Five-Membered Heterocyclic Aromatic Compounds: Overview

4.0K
Heterocyclic aromatic compounds are cyclic compounds that are aromatic and have one or more heteroatoms—atoms other than carbon, in the ring. Depending upon the number of atoms present in the ring, they can be either five or six-membered. Examples of five-membered heterocyclic aromatic compounds include pyrrole, furan, thiophene, and imidazole. Pyrrole consists of one nitrogen atom having one lone pair of electrons. Furan and thiophene have one oxygen and one sulfur heteroatom,...
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相关实验视频

Updated: Jul 17, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
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基于4,5-dihydropyrazolo[1,5-a]quinazoline支架的结构优化,用于改善杀虫活动.

Shuai Yang1, Benjie Li1, Jiahong Tang1

  • 1National Key Laboratory of Green Pesticide, Key Laboratory of Natural Pesticide and Chemical Biology, Ministry of Education, College of Plant Protection, South China Agricultural University, Guangzhou 510642, People's Republic of China.

Pesticide biochemistry and physiology
|September 4, 2023
PubMed
概括

基于4,5-dihydropyrazolo[1,5-a]quinazoline (DPQ) 支架的新型杀虫剂对像Plutella xylostella这样的害虫具有很高的疗效. 化合物12是一种强大的GABA受体对抗剂,具有显著的杀虫活性和农业化学开发潜力.

关键词:
4,5-dihydropyrazolo[1,5-a]quinazoline的使用情况诱 诱 诱 这些昆虫的GABA受体是什么?杀虫剂活动 杀虫剂活动杀虫剂是一种杀虫剂.

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科学领域:

  • 农业化学 农业化学
  • 昆虫毒理学 昆虫毒理学
  • 药品化学 药品化学 是一个

背景情况:

  • 抗昆虫剂耐药性和环境问题需要新的害虫控制剂.
  • 4,5-dihydropyrazolo[1,5-a]quinazoline (DPQ) 支架提供了一种新的作用模式,向没有交叉抵抗的昆虫γ-氨基黄油酸受体 (GABAR).
  • 以前的研究发现,pyraquinil是一种高度杀虫剂DPQ.

研究的目的:

  • 设计和合成新的DPQ衍生物.
  • 评估这些化合物对关键农业害虫的杀虫活性.
  • 调查有前途的候选人的行动方式.

主要方法:

  • 基于pyraquinil的一系列新型DPQ化合物的合成.
  • 对抗Plutella xylostella,Spodoptera exigua,Spodoptera frugiperda和Solenopsis invicta的杀虫活动的评估.
  • 使用Xenopus卵细胞进行电生理学研究,以评估GABAR对抗性.
  • 分子对接和密度函数理论 (DFT) 计算,以了解结构-活动关系.

主要成果:

  • 与现有的杀虫剂如fipronil.com相比,化合物6和12对P.xylostella表现出更高的杀虫活性.
  • 化合物12对Solenopsis invicta具有很高的疗效,在0.5毫克/升的剂量下死亡率为98.89%.
  • 电生理学数据证实化合物12是一种强大的GABAR抗剂.
  • 分子对接揭示了化合物12和P. xylostella GABAR之间的关键相互作用.

结论:

  • 该DPQ支架是开发具有新动作模式的新杀虫剂的有希望的基础.
  • 化合物12具有显著的杀虫剂潜力,值得作为农业化学品候选剂进一步开发.
  • 这项研究为基于DPQ的农药的合理设计提供了宝贵的见解.