新型嘧啶衍生物的设计、合成、体外抗菌和抗氧化评估

Q2 Pharmacology, Toxicology and Pharmaceutics Current Bioactive Compounds Pub Date : 2024-06-06 DOI:10.2174/0115734072301970240528053901
Kaushal Arora, Prabhakar Kumar Verma
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引用次数: 0

摘要

本研究采用 Knovengeal 缩合法制备了一系列新的 2-氨基-6-(取代)嘧啶-4-基-2H-苯并吡喃-2-酮类似物(S1-S15),并对其抗菌和抗氧化活性进行了评估。为了确认这些化合物的化学结构,我们采用了一系列技术,包括FT-IR、MS、1H-NMR 和元素分析。在这一系列化合物中,S1 对金黄色葡萄球菌具有很强的抗菌效果,最低抑菌浓度为 16.26μg/ml;化合物 S7 对枯草杆菌和大肠杆菌具有显著的抗菌潜力,最低抑菌浓度为 17.34μg/ml。在抗真菌活性方面,化合物 S7 和 S11 对黑僵菌的作用最强,最低抑制浓度为 17.34μg/ml。在评估抗氧化活性时,发现化合物 S2 和 S4 显示出突出的抗氧化特性,其 IC50 值分别为 13.33μg/ml 和 43.13μg/ml。通过指定方法进行评估后,新生成的衍生物显示出强大的抗菌和抗氧化特性,在比较分析中超过了常规药物的功效。值得注意的是,化合物 S1、S2、S7、S4 和 S11 甚至比参考药物表现出更高的活性。此外,还讨论了它们的结构-活性关系。
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Design, Synthesis, In vitro Antimicrobial and Antioxidant Evaluation of Novel Pyrimidine Derivatives
In this study, a new series of 2-amino-6-(substituted)pyrimidin-4-yl-2Hchromen- 2-one analogues (S1-S15) was prepared by using the Knovengeal condensation method and evaluated for antimicrobial as well as antioxidant activity. To ensure the progress and confirmation of the reactions, TLC was employed. The melting points (MP) were ascertained utilising a Sunbim-made sonar melting point device produced in India. To confirm the chemical structures of these compounds, we employed a range of techniques, including FT-IR, MS, 1H-NMR, and Elemental analysis. The antimicrobial and antifungal activity was evaluated using the tube dilution method, and a DPPH assay was used to assess antioxidant activity. Within the series, S1 demonstrated strong antibacterial efficacy against S. Aureus, with a minimum inhibitory concentration value of 16.26μg/ml, while compound S7 displayed significant potential against B. subtilis and E. coli, with a MIC value of 17.34μg/ml. For antifungal activity, compounds S7 and S11 are the most potent against A. niger, showing a minimum inhibitory concentration of 17.34μg/ml. In the evaluation of antioxidant activity, it was observed that compounds S2 and S4 displayed outstanding antioxidant properties, with IC50 values of 13.33μg/ml and 43.13μg/ml. The newly created derivatives exhibited robust antimicrobial and antioxidant characteristics upon assessment through designated methodologies, surpassing the efficacy of conventional drugs in the comparative analysis. Notably, compounds S1, S2, S7, S4, and S11 exhibited even greater activity than the reference drugs. Their structure-activity relationship was also discussed.
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来源期刊
Current Bioactive Compounds
Current Bioactive Compounds Pharmacology, Toxicology and Pharmaceutics-Pharmacology, Toxicology and Pharmaceutics (all)
CiteScore
1.90
自引率
0.00%
发文量
112
期刊介绍: The journal aims to provide comprehensive review articles on new bioactive compounds with proven activities in various biological screenings and pharmacological models with a special emphasis on stereoeselective synthesis. The aim is to provide a valuable information source of bioactive compounds synthesized or isolated, which can be used for further development of pharmaceuticals by industry and academia. The journal should prove to be essential reading for pharmacologists, natural product chemists and medicinal chemists who wish to be kept informed and up-to-date with the most important developments on new bioactive compounds of natural or synthetic origin, including their stereoeselective synthesis.
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