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.
Oxoby
Mayalen
M
MUTABILIS SA, Romainville, France.
Moreau
François
F
Durant
Lionel
L
Denis
Alexis
A
Genevard
Jean-Marie
JM
Vongsouthi
Vanida
V
Escaich
Sonia
S
Gerusz
Vincent
V
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