Towards Gram-positive antivirulence drugs: new inhibitors of Streptococcus agalactiae Stk1.
A structure-activity relationship study from a screening hit and structure-based design strategy has led to the identification of bisarylureas as potent inhibitors of Streptococcus agalactiae Stk1. As this target has been directly linked to bacterial virulence, these inhibitors can be considered as a promising step towards antivirulence drugs.
MUTABILIS SA, Romainville, France.
Mayalen
M
Oxoby
François
F
Moreau
Lionel
L
Durant
Alexis
A
Denis
Jean-Marie
JM
Genevard
Vanida
V
Vongsouthi
Sonia
S
Escaich
Vincent
V
Gerusz
D000900:Anti-Bacterial Agents / Q000737:chemistry* / Q000494:pharmacology; D006094:Gram-Positive Bacteria / Q000187:drug effects; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors*; D013292:Streptococcus agalactiae / Q000187:drug effects*; D013329:Structure-Activity Relationship; D014508:Urea / Q000031:analogs & derivatives* / Q000494:pharmacology / Q000627:therapeutic use; D014774:Virulence / Q000187:drug effects
D000900:Anti-Bacterial Agents; D014508:Urea; C474028:Stk1 protein, Streptococcus agalactiae; D017346:Protein Serine-Threonine Kinases