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<p>In recent years, the emergence and propagation of resistant microorganisms have outpaced the introduction of new therapeutic alternatives capable of combating them, giving rise to concerns about an imminent global health crisis caused by infectious diseases. Among the various resistance mechanisms bacteria employ, efflux pumps and β-lactamase enzymes are particularly significant. Consequently, numerous studies have been conducted to identify novel therapeutic alternatives with antibacterial activity and the capacity to inactivate these mechanisms. In this study, a novel (2E)-3-({4-[(2E)-3-(4-nitrophenyl) prop-2-enol] phenyl} carbamoyl) prop-2-enoic acid chalcone, termed CAP, was synthesised. Despite the CAP chalcone exhibiting no direct antibacterial activity and being ineffective against the efflux pump present in the K2068 strain, it was found to potentiate the action of ampicillin when associated with this antibiotic in the K4100 strain, which carries the β-lactamase mechanism. This finding suggests that the chalcone in question could act by inhibiting the resistance mechanism mediated by these enzymes.</p>

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Antibacterial Activity of Chalcone (2E)-3-({4-[(2E)-3-(4-Nitrophenyl) prop-2-enol] phenyl}carbamoyl) prop-2-enoic acid and Its Effect Against Staphylococcus aureus Carrying Efflux Pump and β-Lactamase

  • 期刊论文

  • 发表日期：

    2025年10月24日

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  • Olivia Caroline Maia de Moura,
  • Júlio César Silva,
  • Raimundo Luiz Silva Pereira,
  • Isaac Moura Araújo,
  • Sheila Alves Gonçalves,
  • João Arthur de Oliveira Borges,
  • Daniel Sampaio Alves,
  • Gabriel Gonçalves Alencar,
  • Thiago Sampaio de Freitas,
  • Vanessa Lima-Bezerra,
  • Walber Henrique Ferreira Ribeiro,
  • Francisco Ferdinando Mesquita Cajazeiras,
  • Jesyka Macedo Guedes,
  • Paulo Nogueira Bandeira,
  • Hélcio Silva dos Santos,
  • Henrique Douglas Melo Coutinho,
  • Francisco Nascimento Pereira Junior

摘要

In recent years, the emergence and propagation of resistant microorganisms have outpaced the introduction of new therapeutic alternatives capable of combating them, giving rise to concerns about an imminent global health crisis caused by infectious diseases. Among the various resistance mechanisms bacteria employ, efflux pumps and β-lactamase enzymes are particularly significant. Consequently, numerous studies have been conducted to identify novel therapeutic alternatives with antibacterial activity and the capacity to inactivate these mechanisms. In this study, a novel (2E)-3-({4-[(2E)-3-(4-nitrophenyl) prop-2-enol] phenyl} carbamoyl) prop-2-enoic acid chalcone, termed CAP, was synthesised. Despite the CAP chalcone exhibiting no direct antibacterial activity and being ineffective against the efflux pump present in the K2068 strain, it was found to potentiate the action of ampicillin when associated with this antibiotic in the K4100 strain, which carries the β-lactamase mechanism. This finding suggests that the chalcone in question could act by inhibiting the resistance mechanism mediated by these enzymes.