article · Antibiotics
Rising antibiotic resistance makes the discovery of new antimicrobial compounds essential. To address this challenge, twelve flavonoid molecules, comprising four chalcones, four flavones, and four flavanones, were chemically synthesised with chlorine, bromine, and methoxy modifications. Laboratory evaluation against nine bacterial strains and three fungal strains revealed that most of the compounds showed moderate to high antibacterial activity. Chalcones proved more effective than flavones or flavanones, demonstrating notable potency against Staphylococcus aureus with minimum inhibitory concentrations ranging between 31.25 and 125 micrograms per millilitre. Antifungal activity was also observed, displaying a strong structure-activity relationship. Further cellular analysis showed that a brominated chalcone acted by causing significant membrane permeabilisation and leakage in Staphylococcus aureus cells.
Bacterial resistance to existing antibiotics represents an urgent challenge for modern healthcare. By identifying specific synthetic flavonoid structures that disrupt bacterial membranes, this research reveals potential chemical templates for developing new antimicrobial agents capable of tackling persistent pathogens such as Staphylococcus aureus.
The findings could support pharmaceutical developers and medicinal chemists designing new antimicrobial agents against resistant bacteria and fungi. Because the study is limited to in vitro laboratory screening and mechanistic testing, the work sits at an early discovery stage. Significant further research, including toxicity screening and animal trials, is required before these compounds could be translated into therapeutic products.
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The emergence of antibiotics-resistant bacteria has been a serious concern for medical professionals over the last decade. Therefore, developing new and effective antimicrobials with modified or different modes of action is a continuing imperative. In this context, our study focuses on evaluating the antimicrobial activity of different chemically synthesized flavonoids (FLAV) to guide the chemical synthesis of effective antimicrobial molecules. A set of 12 synthesized molecules (4 chalcones, 4 flavones and 4 flavanones), bearing substitutions with chlorine and bromine groups at the C6′ position and methoxy group at the C4′ position of the B-ring were evaluated for antimicrobial activity toward 9 strains of Gram-positive and Gram-negative bacteria and 3 fungal strains. Our findings showed that most tested FLAV exhibited moderate to high antibacterial activity, particularly against Staphylococcus aureus with minimum inhibitory concentrations (MIC) between the range of 31.25 and 125 μg/mL and that chalcones were more efficient than flavones and flavanones. The examined compounds were also active against the tested fungi with a strong structure-activity relationship (SAR). Interestingly, leakage measurements of the absorbent material at 260 nm and scanning electron microscopy (SEM) demonstrated that the brominated chalcone induced a significant membrane permeabilization of S. aureus.
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DOI: 10.3390/antibiotics12020225
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