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JOURNAL ARTICLE
RESEARCH SUPPORT, N.I.H., EXTRAMURAL
RESEARCH SUPPORT, NON-U.S. GOV'T
Antimicrobial activity of 1,3,4-oxadiazole derivatives against planktonic cells and biofilm of Staphylococcus aureus.
Future Medicinal Chemistry 2018 Februrary
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 μg/ml. At 4 × 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 μg/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.
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 μg/ml. At 4 × 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 μg/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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