article · Scientific Reports
Coumarins are chemical structures known for biological activity, including the ability to stop certain bacteria from forming protective biofilms. Researchers synthesised new hybrid molecules by reacting coumarin-6-sulfonyl chloride and 6-aminocoumarin with various small heterocyclic groups. They then tested these compounds for antimicrobial effects, antibiofilm capabilities, and anti-inflammatory properties. Several derivatives showed strong antimicrobial activity against Staphylococcus aureus, Escherichia coli, Candida albicans, and methicillin-resistant Staphylococcus aureus (MRSA). Among them, compound 9 proved most potent across these pathogens and displayed strong antibiofilm effects, outperforming or matching reference benchmarks. In tests evaluating anti-inflammatory potential in macrophage cells, compound 4d significantly reduced nitric oxide production, achieving 70 percent inhibition and exceeding the performance of the control drug Sulindac.
Bacterial biofilms and resistant pathogens such as MRSA present severe challenges in treating persistent infections. At the same time, chronic inflammation complicates many diseases. Identifying dual-action or highly targeted molecules that suppress microbial biofilms or dampen inflammatory responses provides foundational chemistry that could aid future therapeutic design against complex bacterial infections.
This research provides early-stage laboratory candidates for pharmaceutical developers targeting resistant bacterial infections and inflammatory conditions. The identified compounds could inform the design of future antimicrobial or anti-inflammatory drugs. Because the findings are based entirely on in vitro assays, the work is at a very early stage of research and requires extensive testing and validation before any clinical application.
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Abstract Coumarins are heterocycles of great interest in the development of valuable active structures in chemistry and biological domains. The ability of coumarins to inhibit biofilm formation of Gram positive bacterium ( Staphylococcus aureus ), Gram negative bacterium ( Escherichia coli ) as well as the methicillin-resistant S. aureus (MRSA) has been previously described. In the present work, new hybrid coumarin-heterocycles have been synthesized via the reaction of coumarin-6-sulfonyl chloride and 6-aminocoumarin with different small heterocycle moieties. The biological efficacy of the new compounds was evaluated towards their ability to inhibit biofilm formation and their anti-inflammatory properties. The antimicrobial activities of the newly synthesized compounds were tested against Gram positive bacterium ( S. aureus ATCC 6538), Gram negative bacterium ( E. coli ATCC 25922), yeast ( Candida albicans ATCC 10231) and the fungus ( Aspergillus niger NRRL-A326). Compounds 4d , 4e , 4f , 6a and 9 showed significant MIC and MBC values against S. aureus , E. coli , C. albicans , and methicillin-resistant S. aureus (MRSA) with especial incidence on compound 9 which surpasses all the other compounds giving MIC and MBC values of (4.88 and 9.76 µg/mL for S. aureus ), (78.13 and 312.5 µg/mL for E. coli ), (9.77 and 78.13 µg/mL for C. albicans ), and (39.06 and 76.7 µg/mL for MRSA), respectively. With reference to the antibiofilm activity, compound 9 exhibited potent antibiofilm activity with IC 50 of 60, 133.32, and 19.67 µg/mL against S. aureus, E. coli, and MRSA, (respectively) considering the reference drug (neomycin). Out of all studied compounds, the anti-inflammatory results indicated that compound 4d effectively inhibited nitric oxide production in lipopolysaccharide-(LPS-) stimulated RAW264.7 macrophage cells, giving NO% inhibition of 70% compared to Sulindac (55.2%)
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DOI: 10.1038/s41598-024-59072-w
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