Zhaojun Zheng1,2, Qingzhong Liu1,3, Wooseong Kim1, Nagendran Tharmalingam1, Beth Burgwyn Fuchs1, Eleftherios Mylonakis1. 1. Division of Infectious Diseases, Rhode Island Hospital, Alpert Medical School of Brown University, Providence, RI 02903, USA. 2. State Key Laboratory of Animal Nutrition, College of Animal Science & Technology, China Agricultural University, Beijing 100193, PR China. 3. Department of Clinical Laboratory, Shanghai General Hospital, School of Medicine, Shanghai Jiaotong University, Shanghai 200080, PR China.
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.
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.
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