TY - JOUR
T1 - Antimicrobial activity of 1,3,4-oxadiazole derivatives against planktonic cells and biofilm of Staphylococcus aureus
AU - Zheng, Zhaojun
AU - Liu, Qingzhong
AU - Kim, Wooseong
AU - Tharmalingam, Nagendran
AU - Fuchs, Beth Burgwyn
AU - Mylonakis, Eleftherios
N1 - Publisher Copyright:
© 2018 Newlands Press.
PY - 2018/2
Y1 - 2018/2
N2 - 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.
AB - 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.
KW - 1,3,4-oxadiazole derivatives
KW - Staphylococcus aureus
KW - antibiotic resistance
KW - biofilm
KW - planktonic cells
UR - http://www.scopus.com/inward/record.url?scp=85041962850&partnerID=8YFLogxK
U2 - 10.4155/fmc-2017-0159
DO - 10.4155/fmc-2017-0159
M3 - Article
C2 - 29334249
AN - SCOPUS:85041962850
SN - 1756-8919
VL - 10
SP - 283
EP - 296
JO - Future Medicinal Chemistry
JF - Future Medicinal Chemistry
IS - 3
ER -