W. F. He, J. X. Wang, P. Y. Gao, D. Q. Li, H. Jin, C. F. Liu, X. G. Liu
{"title":"Design, Synthesis, and Activity Evaluation of Endogenous Hydrogen Sulfide Inhibitor of MRSA","authors":"W. F. He, J. X. Wang, P. Y. Gao, D. Q. Li, H. Jin, C. F. Liu, X. G. Liu","doi":"10.1134/S1070363224612638","DOIUrl":null,"url":null,"abstract":"<p>Eighteen indole target compounds were synthesized from 3-(6-bromo-3-indolyl)propionic acid. The chemical structures were determined by <sup>1</sup>H NMR, <sup>13</sup>C NMR, and HRMS. Bioactivity assays revealed that 3-(6-bromo-3-indolyl)-<i>N</i>-(3-fluorophenyl)propenamide exhibited the most potent inhibitory effect on methicillin-resistant <i>Staphylococcus aureus</i> (MRSA) endogenous H<sub>2</sub>S at a concentration of 40 μM, with an inhibitory rate of 80.2±0.92%. The results of antibacterial experiments showed that co-administering partial target compounds with oxacillin sodium reduced the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of MRSA by 50% when compared to oxacillin sodium alone. Further studies revealed that the synergistic antimicrobial mechanism is closely related to the Fenton reaction. The results of the cytotoxicity assay showed that 3-(6-bromo-3-indolyl)-<i>N</i>-(4-chlorobenzyl)propenamide had the least inhibitory effect on BEAS-2B cells. The experimental results of this study may provide references and ideas for the treatment of MRSA infection.</p>","PeriodicalId":761,"journal":{"name":"Russian Journal of General Chemistry","volume":"95 3","pages":"606 - 619"},"PeriodicalIF":0.8000,"publicationDate":"2025-03-27","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Russian Journal of General Chemistry","FirstCategoryId":"92","ListUrlMain":"https://link.springer.com/article/10.1134/S1070363224612638","RegionNum":4,"RegionCategory":"化学","ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"Q4","JCRName":"CHEMISTRY, MULTIDISCIPLINARY","Score":null,"Total":0}
引用次数: 0
Abstract
Eighteen indole target compounds were synthesized from 3-(6-bromo-3-indolyl)propionic acid. The chemical structures were determined by 1H NMR, 13C NMR, and HRMS. Bioactivity assays revealed that 3-(6-bromo-3-indolyl)-N-(3-fluorophenyl)propenamide exhibited the most potent inhibitory effect on methicillin-resistant Staphylococcus aureus (MRSA) endogenous H2S at a concentration of 40 μM, with an inhibitory rate of 80.2±0.92%. The results of antibacterial experiments showed that co-administering partial target compounds with oxacillin sodium reduced the minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) of MRSA by 50% when compared to oxacillin sodium alone. Further studies revealed that the synergistic antimicrobial mechanism is closely related to the Fenton reaction. The results of the cytotoxicity assay showed that 3-(6-bromo-3-indolyl)-N-(4-chlorobenzyl)propenamide had the least inhibitory effect on BEAS-2B cells. The experimental results of this study may provide references and ideas for the treatment of MRSA infection.
期刊介绍：
Russian Journal of General Chemistry is a journal that covers many problems that are of general interest to the whole community of chemists. The journal is the successor to Russia’s first chemical journal, Zhurnal Russkogo Khimicheskogo Obshchestva (Journal of the Russian Chemical Society ) founded in 1869 to cover all aspects of chemistry. Now the journal is focused on the interdisciplinary areas of chemistry (organometallics, organometalloids, organoinorganic complexes, mechanochemistry, nanochemistry, etc.), new achievements and long-term results in the field. The journal publishes reviews, current scientific papers, letters to the editor, and discussion papers.
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