Journal
FUTURE MEDICINAL CHEMISTRY
Volume 10, Issue 3, Pages 283-296Publisher
FUTURE SCI LTD
DOI: 10.4155/fmc-2017-0159
Keywords
1,3,4-oxadiazole derivatives; antibiotic resistance; biofilm; planktonic cells; Staphylococcus aureus
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Funding
- NIH [P01 AI083214]
- China Scholarship Council through Chinese Government Graduate Student Overseas Study Program
- Shanghai General Hospital Characteristic Discipline Construction Fund
- Shanghai Jiao Tong University K C Wong Medical Fellowship Fund
- NATIONAL INSTITUTE OF ALLERGY AND INFECTIOUS DISEASES [P01AI083214] Funding Source: NIH RePORTER
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Aim: Staphylococcus aureus is a major cause of severe hospital-acquired infections, and biofilm formation is an important part of staphylococcal pathogenesis. Therefore, developing new antimicrobial agents against both planktonic cells and biofilm of S. aureus is a major challenge. Results: Three 1,3,4-oxadiazole derivatives exhibited antimicrobial activity against seven S. aureus strains in vitro, with minimum inhibitory concentrations ranging from 4 to 32 mu g/ml. At 4 x minimum inhibitory concentration, all compounds killed cells within 24 h, demonstrating bactericidal activity. In addition to their effects against planktonic cells, these compounds prevented biofilm formation in a dose-dependent manner, with inhibitory concentrations for biofilm formation ranging from 8 to 32 mu g/ml. Interestingly, higher concentrations of these compounds were effective against mature biofilms and all compounds downregulated the transcription of the biofilm-related gene spa. Conclusion: We report three new 1,3,4-oxadiazole derivatives that have bactericidal activity and could provide as alternatives to combat S. aureus.
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