{"title":"新型嘧啶衍生物的设计、合成、体外抗菌和抗氧化评估","authors":"Kaushal Arora, Prabhakar Kumar Verma","doi":"10.2174/0115734072301970240528053901","DOIUrl":null,"url":null,"abstract":"\n\nIn this study, a new series of 2-amino-6-(substituted)pyrimidin-4-yl-2Hchromen-\n2-one analogues (S1-S15) was prepared by using the Knovengeal condensation method\nand evaluated for antimicrobial as well as antioxidant activity.\n\n\n\nTo ensure the progress and confirmation of the reactions, TLC was employed. The melting\npoints (MP) were ascertained utilising a Sunbim-made sonar melting point device produced in India.\nTo confirm the chemical structures of these compounds, we employed a range of techniques, including\nFT-IR, MS, 1H-NMR, and Elemental analysis. The antimicrobial and antifungal activity was\nevaluated using the tube dilution method, and a DPPH assay was used to assess antioxidant activity.\n\n\n\nWithin 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.\n\n\n\nThe newly created derivatives exhibited robust antimicrobial and antioxidant characteristics\nupon assessment through designated methodologies, surpassing the efficacy of conventional\ndrugs in the comparative analysis. Notably, compounds S1, S2, S7, S4, and S11 exhibited even\ngreater activity than the reference drugs. Their structure-activity relationship was also discussed.\n","PeriodicalId":10772,"journal":{"name":"Current Bioactive Compounds","volume":"22 46","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2024-06-06","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"Design, Synthesis, In vitro Antimicrobial and Antioxidant Evaluation of\\nNovel Pyrimidine Derivatives\",\"authors\":\"Kaushal Arora, Prabhakar Kumar Verma\",\"doi\":\"10.2174/0115734072301970240528053901\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"\\n\\nIn this study, a new series of 2-amino-6-(substituted)pyrimidin-4-yl-2Hchromen-\\n2-one analogues (S1-S15) was prepared by using the Knovengeal condensation method\\nand evaluated for antimicrobial as well as antioxidant activity.\\n\\n\\n\\nTo ensure the progress and confirmation of the reactions, TLC was employed. The melting\\npoints (MP) were ascertained utilising a Sunbim-made sonar melting point device produced in India.\\nTo confirm the chemical structures of these compounds, we employed a range of techniques, including\\nFT-IR, MS, 1H-NMR, and Elemental analysis. The antimicrobial and antifungal activity was\\nevaluated using the tube dilution method, and a DPPH assay was used to assess antioxidant activity.\\n\\n\\n\\nWithin 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.\\n\\n\\n\\nThe newly created derivatives exhibited robust antimicrobial and antioxidant characteristics\\nupon assessment through designated methodologies, surpassing the efficacy of conventional\\ndrugs in the comparative analysis. Notably, compounds S1, S2, S7, S4, and S11 exhibited even\\ngreater activity than the reference drugs. Their structure-activity relationship was also discussed.\\n\",\"PeriodicalId\":10772,\"journal\":{\"name\":\"Current Bioactive Compounds\",\"volume\":\"22 46\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2024-06-06\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Current Bioactive Compounds\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.2174/0115734072301970240528053901\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"Q2\",\"JCRName\":\"Pharmacology, Toxicology and Pharmaceutics\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Current Bioactive Compounds","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.2174/0115734072301970240528053901","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q2","JCRName":"Pharmacology, Toxicology and Pharmaceutics","Score":null,"Total":0}
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.
Current Bioactive CompoundsPharmacology, 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.