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The Antimicrobial and Cytotoxicity Properties of New Dibrominated 1,3-Dithiolium Flavonoids
Laura Gabriela Sarbu1, Ana Alexandra Dumitru2, Mihaela Savu2
1Department of Chemistry, Alexandru Ioan Cuza University of Iasi, Bd. Carol I, No. 11, 700506 Iasi, Romania.
Abstract:
Background/Objectives: Antimicrobial resistance (AMR) presents a medical risk as well as a significant global socioeconomic challenge. Key contributors to AMR include the excessive use and incorrect application of antibiotics in humans and agriculture, nosocomial infections, and the absence of new classes of antibiotics. Methods: Novel dibrominated tricyclic flavonoids have been synthesized from the corresponding 3-dithiocarbamic flavanones and their antimicrobial and cytotoxicity properties have been investigated. Results: It has been found that these tricyclic flavonoids exhibit strong antimicrobial properties against clinically relevant pathogens such as Staphylococcus aureus, Acinetobacter baumannii, and Escherichia coli with MIC and MBC values against S. aureus ATCC 25923 as low as 0.12 µg/mL and 1.9 µg/mL, respectively. Conclusions: The synthetic tricyclic flavonoids exhibit strong antibacterial activity against selected WHO priority pathogens, including Staphylococcus aureus and Acinetobacter baumannii, surpassing the efficacy of both natural and synthetic flavonoids and several conventional antibiotics.
Insights
Novel synthetic tricyclic flavonoids show potent antimicrobial activity against priority pathogens like Staphylococcus aureus and Acinetobacter baumannii. These compounds offer a promising new avenue for combating antimicrobial resistance (AMR).
Area of Science:
- Medicinal Chemistry
- Organic Synthesis
- Microbiology
Background:
- Antimicrobial resistance (AMR) is a major global health and socioeconomic challenge.
- Contributing factors include antibiotic overuse, nosocomial infections, and a lack of new antibiotic classes.
- Addressing AMR requires the development of novel antimicrobial agents.
Purpose of the Study:
- To synthesize novel dibrominated tricyclic flavonoids.
- To investigate the antimicrobial properties of these novel compounds.
- To evaluate their cytotoxicity.
Main Methods:
- Synthesis of novel dibrominated tricyclic flavonoids from 3-dithiocarbamic flavanones.
- Antimicrobial activity testing against clinically relevant pathogens.
- Cytotoxicity assays.
Main Results:
- The synthesized tricyclic flavonoids demonstrated significant antimicrobial activity.
- Potent activity was observed against Staphylococcus aureus, Acinetobacter baumannii, and Escherichia coli.
- MIC and MBC values against S. aureus ATCC 25923 were as low as 0.12 µg/mL and 1.9 µg/mL, respectively.
Conclusions:
- Synthetic tricyclic flavonoids possess strong antibacterial activity against WHO priority pathogens.
- These compounds exhibit superior efficacy compared to natural/synthetic flavonoids and some conventional antibiotics.
- The findings highlight the potential of these novel flavonoids in combating AMR.
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