新型四甲-1--乙尿素:合成和双抗菌-抗癌活动
Yusuf Akbaba1, Fatma Necmiye Kacı2,3, Mehmet Enes Arslan4
1Department of Basic Sciences, Faculty of Science, Erzurum Technical University, Erzurum, Turkey.
Journal of enzyme inhibition and medicinal chemistry
|December 8, 2023
概括
这项研究开发了新型尿素衍生物,显示出强大的抗菌和抗癌特性. 这些化合物有效地向癌细胞,同时对健康细胞具有较低的毒性,为双重作用疗法提供了潜力.
科学领域:
- 药用化学 医学化学
- 有机合成 有机合成
- 药理学 药理学是指药理学的学科.
背景情况:
- 癌症和抗生素耐药性细菌感染对全球健康构成重大威胁.
- 在癌症治疗过程中形成的抗药性加剧了治疗挑战.
研究的目的:
- 合成和评估新型N,N'-二甲基尿素衍生物的联合抗癌和抗菌活性.
- 评估合成化合物的细胞毒性,以对抗各种癌细胞系和细菌菌株.
主要方法:
- 使用异酸盐化学合成N,N'-二基尿素衍生物.
- 通过最小抑制度 (MIC) 测定来评估抗菌活性.
- 对人类癌细胞系 (HeLa,SH-SY5Y) 和健康的纤维细胞细胞毒性的评估.
主要成果:
- 合成的14-18化合物产量为73-76%.
- 所有衍生品都表现出强烈的抗菌活性,MIC值在0.97~15.82μM之间.
- 化合物14和16对HeLa细胞具有很高的疗效;化合物14,15和17对SH-SY5Y细胞具有活性.
- 合成的化合物表现出选择性毒性,对健康的纤维细胞比癌细胞的危害要小.
结论:
- 合成的尿素衍生物具有显著的双作用潜力,可以对抗癌症和细菌感染.
- 14,15,16和17的化合物代表了开发具有更好的安全性概况的新治疗剂的有希望的线索.
更多相关视频
10:42Preparation of N-2-alkoxyvinylsulfonamides from N-tosyl-1,2,3-triazoles and Subsequent Conversion to Substituted Phthalans and Phenethylamines
Published on: January 3, 2018
9.8K
07:12Cercosporin-Photocatalyzed [4+1]- and [4+2]-Annulations of Azoalkenes Under Mild Conditions
Published on: July 17, 2020
6.3K
相关概念视频
Physical Properties of Amines
3.2K
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.
3.2K
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
Preparation of 1° Amines: Gabriel Synthesis
3.6K
Direct alkylation is not a suitable method for synthesizing amines because it produces polyalkylated products. Gabriel synthesis is the most preferred method to exclusively make primary amines. The method uses phthalimide, which contains a protected form of nitrogen that participates in alkylation only once to predominantly give primary amines.
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
Strong bases like NaOH or KOH deprotonate the phthalimide to form the corresponding anion, which acts as a nucleophile. Further, the anion attacks an...
3.6K
Combined Effects of Drugs: Synergism
3.9K
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...
3.9K
