作为抗菌剂的二二二二醇合N-piperazinyl乙胺:设计,合成,生物评估和分子对接研究
Rakesh K Bollikanda1,2, Devendra Nagineni1,2, Abburi Naga Pranathi1,2
1Fluoro & Agrochemicals Division, CSIR-Indian Institute of Chemical Technology, Hyderabad, Telangana, India.
Archiv der Pharmazie
|November 30, 2023
概括
新型N-异环化合物被合成并测试其抗微生物活性. 几种化合物显示出有前途的抗菌,抗真菌和抗结核作用,突出了它们作为新药候选者的潜力.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 抗微生物药物发现发现
背景情况:
- 替代的和N-异循环是药物开发中的越来越重要的支架.
- 抗微生物耐药性需要发现新的治疗药物.
研究的目的:
- 为了合成和评估抗微生物活性的新型本佐提亚-皮佩拉衍生物.
- 探索这些化合物作为药理活性框架的潜力.
主要方法:
- 采用了三步合成,从循环的1,3-二和氨酸开始.
- 新型乙胺衍生物 (7a-af) 通过NMR和质谱学进行合成和表征.
- 进行了体外抗菌检测,对抗细菌和真菌菌株,包括Mycobacterium tuberculosis.
主要成果:
- 合成了32种新型化合物,产量很好.
- 化合物7c和7l表现出抗真菌活性;类似物7d,7l,7n和7r表现出强烈的抗菌作用.
- 化合物7j,7l和7w对Mycobacterium tuberculosis H37Rv.表现出适度的抗结核活性.
结论:
- 合成的索-皮佩拉辛支架是开发新抗菌剂的有希望的框架.
- 进一步的研究,包括分子对接和ADMET预测,支持这些化合物的潜力.
相关概念视频
Basicity of Heterocyclic Aromatic Amines
6.0K
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).
6.0K
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 with Halogens and Cyanide: Sandmeyer and Schiemann Reactions
1.9K
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...
1.9K
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


