Antimicrobial activity of 1,3,4-oxadiazole derivatives against planktonic cells and biofilm of Staphylococcus aureus

Zhaojun Zheng, Qingzhong Liu, Wooseong Kim, Nagendran Tharmalingam, Beth Burgwyn Fuchs, Eleftherios Mylonakis

Research output: Contribution to journalArticlepeer-review

35 Scopus citations

Abstract

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.

Original languageEnglish
Pages (from-to)283-296
Number of pages14
JournalFuture Medicinal Chemistry
Volume10
Issue number3
DOIs
StatePublished - Feb 2018

Keywords

  • 1,3,4-oxadiazole derivatives
  • Staphylococcus aureus
  • antibiotic resistance
  • biofilm
  • planktonic cells

Fingerprint

Dive into the research topics of 'Antimicrobial activity of 1,3,4-oxadiazole derivatives against planktonic cells and biofilm of Staphylococcus aureus'. Together they form a unique fingerprint.

Cite this