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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>

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Design, Synthesis, and Activity Evaluation of Endogenous Hydrogen Sulfide Inhibitor of MRSA

  • 期刊论文

  • 发表日期：

    2025年3月27日

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  • W. F. He,
  • J. X. Wang,
  • P. Y. Gao,
  • D. Q. Li,
  • H. Jin,
  • C. F. Liu,
  • X. G. Liu

摘要

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.