相关实验视频
Updated: May 31, 2025

11:51
Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
11.8K
合成一些thiazolyl和Oxazolyl Quinazoline衍生物作为潜在的抗微生物剂
Krishana Kumar Sharma1, Gandharve Kumar2, Shoma Devi3
1Department of Pharmacology, Teerthanker Mahaveer College of Pharmacy, Teerthanker Mahaveer University, Moradabad (UP), 244001, India.
Current organic synthesis
|January 23, 2025
概括
新合成的奎纳林衍生物显示出强大的抗菌和抗真菌活性. 与现有药物相比,3c'化合物表现出更高的疗效,突出了其在药物化学中的潜力.
科学领域:
- 药用化学 医学化学
- 异环化学 异环化学
- 药物发现 药物发现 药物发现
背景情况:
- 奎纳林衍生物在制药化学中至关重要,是众多药物和生物活性化合物的基础.
- 含有N的异环基纳林表现出多种生物制药活动.
研究的目的:
- 为了合成基于quinazoline的新型异环化合物.
- 评估这些新化合物的抗菌和抗真菌特性.
- 为了比较它们与已确定的抗微生物药物的疗效.
主要方法:
- 合成N-(4-替代的zylidene)-2-(2-aminothiazol-4-yl)-6-methylquinazolin-3(4H) - amines (3a'-3e') 和N-(4-替代的zylidene)-2-(2-aminooxazol-4-yl)-6-methylquinazolin-3(4H) - amines (3a-3e) 的合成方法.
- 对抗菌和抗真菌活性进行评估.
- 与伊米佩内姆和米可纳的比较分析.
主要成果:
- 化合物3c'显示出显著的抗菌和抗真菌潜力.
- 合成的化合物被评估为它们的抗微生物疗效.
- 化合物3c'在抗微生物试验中表现优于其他新型化合物和标准药物.
结论:
- 合成化合物的结构使用元素分析 (C.H.N.) 得到证实. 和光谱技术 (1H NMR,13C NMR,IR,GCMS). 在这种情况下,
- 该研究成功地确定了一种具有显著抗菌活性的有前途的quinazoline衍生物 (3c').
相关概念视频
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
2.9K
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...
2.9K
Diazonium Group Substitution: –OH and –H
2.7K
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.
2.7K
Diazonium Group Substitution with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
1.8K
Arenediazonium substitution reactions occur when the diazonium group is substituted by various functional groups such as halides, hydroxyl, nitrile, etc. For instance, arenediazonium salts react with copper(I) salts of chloride, bromide, or cyanide to form corresponding aryl chlorides, bromides, and nitriles. These reactions are named Sandmeyer reactions. Although the mechanism of this reaction is complicated, as illustrated in Figure 1, they are believed to progress via an aryl copper...
1.8K
Oxidation of Phenols to Quinones
2.8K
In the presence of oxidizing agents, phenols are oxidized to quinones. Quinones can be easily reduced back to phenols using mild reducing agents. The electron-donating hydroxyl group enhances the reactivity of the aromatic ring, enabling oxidation of the ring even in the absence of an α hydrogen.
o-hydroxy phenols are oxidized to o-quinones and p-hydroxy phenols to p-quinones. Such redox reactions involve the transfer of two electrons and two protons. The reversible redox...
o-hydroxy phenols are oxidized to o-quinones and p-hydroxy phenols to p-quinones. Such redox reactions involve the transfer of two electrons and two protons. The reversible redox...
2.8K
Preparation of 1° Amines: Azide Synthesis
3.8K
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...
3.8K
Combined Effects of Drugs: Synergism
3.7K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
3.7K

![Solid-phase Synthesis of [4.4] Spirocyclic Oximes](/_next/image?url=https%3A%2F%2Fcloudfront.jove.com%2FCDNSource%2Fteasers%2F58508.jpg&w=3840&q=50)