一些含有脱辛格龙片段的2,4-二基托的合成,表征和生物活性:DNA和蛋白质结合研究研究
Kristina Mihajlović1, Nenad Joksimović1, Nenad Janković2
1University of Kragujevac, Faculty of Science, Department of Chemistry, Radoja Domanovića 12, 34000 Kragujevac, Serbia.
Bioorganic & medicinal chemistry letters
|July 27, 2023
概括
新的2,4-二基基 Ester 显示出强大的抗微生物和抗真菌活性. 这些化合物还有效地与牛血清白蛋白结合,并与DNA相互作用,表明临床应用的潜力.
科学领域:
- 药用化学 医学化学
- 药理学 药理学是指药理学的学科.
- 生物化学 生物化学
背景情况:
- 抗生素耐药性是一个日益严重的全球健康问题,需要发现新型抗菌剂.
- 探索新药的各种来源对于对抗耐药细菌菌株至关重要.
研究的目的:
- 为了合成和评估一系列的2,4-diketo 的抗微生物和抗真菌性质.
- 研究这些化合物的与牛血清白蛋白和DNA的结合相互作用.
- 通过分子对接来评估潜在的抗瘤活性和结合机制.
主要方法:
- 合成2,4-二甲基酸的合成.
- 抗菌和抗真菌活性测定对各种细菌菌株和真菌.
- 光谱学用于研究化合物-DNA相互作用.
- 用DNA和牛血清白蛋白进行结合模式分析的分子对接模拟.
主要成果:
- 两种合成的化合物表现出显著的抗菌活性,对抗黄金葡萄球菌和细菌细菌.
- 三植物 (Trichophyton mentagrophytes) 对测试的化合物表现出高度的敏感性.
- 所有化合物都表现出对牛血清专蛋白具有适当的结合亲和力.
- 大多数化合物通过介质与DNA相互作用,表明潜在的抗瘤特性.
结论:
- 合成的2,4-diketo 具有有前途的抗微生物,抗真菌和潜在的抗瘤活性.
- 与牛血清白蛋白和DNA的有利结合相互作用支持它们的治疗潜力.
- 这些化合物代表了一种潜在的新类药物,可用于临床应用,用于对抗感染和可能的癌症.
相关概念视频
Alkylation of β-Diester Enolates: Malonic Ester Synthesis
3.5K
Malonic ester synthesis is a method to obtain α substituted carboxylic acids from ꞵ-diesters such as diethyl malonate and alkyl halides.
3.5K
Intramolecular Claisen Condensation of Dicarboxylic Esters: Dieckmann Cyclization
2.5K
Dieckmann cyclization is an intramolecular Claisen condensation of diesters. The reaction occurs in the presence of a base and generates a cyclic β-ketoester as the final product. Commonly, 1, 6 and 1, 7-diesters are preferred substrates for the reaction since the generated five, and six-membered cyclic β-keto esters are particularly more stable.
2.5K
Alkylation of β-Ketoester Enolates: Acetoacetic Ester Synthesis
3.4K
Acetoacetic ester synthesis is a method to obtain ketones from alkyl halides and β-keto esters. The reaction occurs in the presence of an alkoxide base that abstracts the acidic proton of the β-keto esters. The step results in an enolate ion which is doubly stabilized. The enolate then reacts with an alkyl halide via the SN2 process to produce an alkylated ester intermediate with a new C–C bond. The hydrolysis of the intermediate, followed by acidification, results in an...
3.4K
β-Dicarbonyl Compounds via Crossed Claisen Condensations
3.2K
Crossed Claisen condensations are base-promoted reactions between two different ester molecules producing β-dicarbonyl compounds. The reaction involving esters, with both containing α hydrogen, results in a mixture of four different products that are difficult to isolate. This reduces the synthetic utility of the reaction.
3.2K
Esters to β-Ketoesters: Claisen Condensation Mechanism
3.7K
Regular Claisen condensation involves the synthesis of β-ketoesters by combining identical ester molecules bearing two α hydrogens in the presence of an alkoxide base. The reaction commences with the deprotonation of the acidic α hydrogen by the base to form a resonance stabilized ester enolate. This nucleophilic ion then attacks the carbonyl center of another ester molecule to generate a tetrahedral alkoxide intermediate. Next, the expulsion of the alkoxide group from the...
3.7K
Carboxylic Acids to Methylesters: Alkylation using Diazomethane
2.2K
Carboxylic acids react with diazomethane in an ether solvent via alkylation at the carboxylate oxygen atom to give methyl esters of the corresponding acid with excellent yields.
2.2K


