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Synthesis, spectroscopic characterization, and antibacterial activity of chalcone (2E)‐1‐(3′‐aminophenyl)‐3‐(4‐dimethylaminophenyl)‐prop‐2‐en‐1‐one against multiresistant Staphylococcus aureus carrier of efflux pump mechanisms and β‐lactamase

Silva, Larissa ; Donato, Isydório Alves ; Bezerra, Suieny Rodrigues ; Santos, Hélcio Silva ; Bandeira, Paulo Nogueira ; Nascimento, Maria Thalia Ramos ; Guedes, Jesyka Macêdo ; Freitas, Priscila Ramos ; Araújo, Ana Carolina Justino ; Freitas, Thiago Sampaio ; Coutinho, Henrique Douglas Melo ; Matos, Yedda Maria Lobo Soares ; Oliveira, Lígia Cláudia Castro ; Cunha, Francisco Assis Bezerra

Fundamental & clinical pharmacology, 2024-02, Vol.38 (1), p.60-71 [Periódico revisado por pares]

England: Wiley Subscription Services, Inc

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Título:
Synthesis, spectroscopic characterization, and antibacterial activity of chalcone (2E)‐1‐(3′‐aminophenyl)‐3‐(4‐dimethylaminophenyl)‐prop‐2‐en‐1‐one against multiresistant Staphylococcus aureus carrier of efflux pump mechanisms and β‐lactamase
Autor: Silva, Larissa ; Donato, Isydório Alves ; Bezerra, Suieny Rodrigues ; Santos, Hélcio Silva ; Bandeira, Paulo Nogueira ; Nascimento, Maria Thalia Ramos ; Guedes, Jesyka Macêdo ; Freitas, Priscila Ramos ; Araújo, Ana Carolina Justino ; Freitas, Thiago Sampaio ; Coutinho, Henrique Douglas Melo ; Matos, Yedda Maria Lobo Soares ; Oliveira, Lígia Cláudia Castro ; Cunha, Francisco Assis Bezerra
Assuntos: Adaptability ; Anti-Bacterial Agents - pharmacology ; Antibacterial activity ; antibacterial drugs ; Anticancer properties ; Antimicrobial activity ; Bacteria ; Bacterial Proteins - metabolism ; beta-Lactamases - metabolism ; Chalcone - metabolism ; Chalcone - pharmacology ; Chalcones - pharmacology ; Diabetes mellitus ; Drug resistance ; Efflux ; EPIs ; Ethidium - metabolism ; Ethidium - pharmacology ; Ethidium bromide ; infections ; Magnetic properties ; Microbial Sensitivity Tests ; Microbiological assaying ; Minimum inhibitory concentration ; Multidrug Resistance-Associated Proteins ; Natural products ; NMR ; Nomenclature ; Nuclear magnetic resonance ; resistance ; Spectroscopy ; Staphylococcus aureus ; Synthesis
É parte de: Fundamental & clinical pharmacology, 2024-02, Vol.38 (1), p.60-71
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SourceType-Scholarly Journals-1
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Descrição: Background The bacterium Staphylococcus aureus has stood out for presenting a high adaptability, acquiring resistance to multiple drugs. The search for natural or synthetic compounds with antibacterial properties capable of reversing the resistance of S. aureus is the main challenge to be overcome today. Natural products such as chalcones are substances present in the secondary metabolism of plants, presenting important biological activities such as antitumor, antidiabetic, and antimicrobial activity. Objectives In this context, the aim of this work was to synthesize the chalcone (2E)‐1‐(3'‐aminophenyl)‐3‐(4‐dimethylaminophenyl)‐prop‐2‐en‐1‐one with nomenclature CMADMA, confirm its structure by nuclear magnetic resonance (NMR), and evaluate its antibacterial properties. Methods The synthesis methodology used was that of Claisen‐Schmidt, and spectroscopic characterization was performed by NMR. For microbiological assays, the broth microdilution methodology was adopted in order to analyze the antibacterial potential of chalcones and to analyze their ability to act as a possible inhibitor of β‐lactamase and efflux pump resistance mechanisms, present in S. aureus strain K4100. Results The results obtained show that CMADMA does not show direct antibacterial activity, expressing a MIC of ≥1024 μg/mL, or on the enzymatic mechanism of β‐lactamase; however, when associated with ethidium bromide in efflux pump inhibition assays, CMADMA showed promising activity by reducing the MIC of the bromide from 64 to 32 μg/mL. Conclusion We conclude that the chalcone synthesized in this study is a promising substance to combat bacterial resistance, possibly acting in the inhibition of the QacC efflux pump present in S. aureus strain K4100, as evidenced by the reduction in the MIC of ethidium bromide.
Editor: England: Wiley Subscription Services, Inc
Idioma: Inglês

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Synthesis, spectroscopic characterization, and antibacterial activity of chalcone (2E)‐1‐(3′‐aminophenyl)‐3‐(4‐dimethylaminophenyl)‐prop‐2‐en‐1‐one against multiresistant Staphylococcus aureus carrier of efflux pump mechanisms and β‐lactamase

England: Wiley Subscription Services, Inc

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