Aryl rhodanines specifically inhibit staphylococcal and enterococcal biofilm formation.
Staphylococcus epidermidis and Staphylococcus aureus are the leading causative agents of indwelling medical device infections because of their ability to form biofilms on artificial surfaces. Here we describe the antibiofilm activity of a class of small molecules, the aryl rhodanines, which specifically inhibit biofilm formation of S. aureus, S. epidermidis, Enterococcus faecalis, E. faecium, and E. gallinarum but not the gram-negative species Pseudomonas aeruginosa or Escherichia coli. The aryl rhodanines do not exhibit antibacterial activity against any of the bacterial strains tested and are not cytotoxic against HeLa cells. Preliminary mechanism-of-action studies revealed that the aryl rhodanines specifically inhibit the early stages of biofilm development by preventing attachment of the bacteria to surfaces.
Opperman
Timothy J
TJ
Microbiotix, Inc., Worcester, MA 01605, USA. topperman@microbiotix.com
Kwasny
Steven M
SM
Williams
John D
JD
Khan
Atiyya R
AR
Peet
Norton P
NP
Moir
Donald T
DT
Bowlin
Terry L
TL
D000900:Anti-Bacterial Agents / Q000737:chemistry / Q000494:pharmacology; D018441:Biofilms / Q000187:drug effects* / Q000254:growth & development; D016983:Enterococcus / Q000187:drug effects* / Q000254:growth & development*; D013293:Enterococcus faecalis / Q000187:drug effects / Q000254:growth & development; D016984:Enterococcus faecium / Q000187:drug effects / Q000254:growth & development; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D012236:Rhodanine / Q000031:analogs & derivatives* / Q000737:chemistry / Q000494:pharmacology*; D013210:Staphylococcus / Q000187:drug effects* / Q000254:growth & development*; D013211:Staphylococcus aureus / Q000187:drug effects / Q000254:growth & development; D013212:Staphylococcus epidermidis / Q000187:drug effects / Q000254:growth & development
D000900:Anti-Bacterial Agents; D012236:Rhodanine