Towards Gram-positive antivirulence drugs: new inhibitors of Streptococcus agalactiae Stk1

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3486-90. doi: 10.1016/j.bmcl.2010.04.150.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry*
  • Anti-Bacterial Agents / pharmacology
  • Gram-Positive Bacteria / drug effects
  • Protein Serine-Threonine Kinases / antagonists & inhibitors*
  • Streptococcus agalactiae / drug effects*
  • Structure-Activity Relationship
  • Urea / analogs & derivatives*
  • Urea / pharmacology
  • Urea / therapeutic use
  • Virulence / drug effects

Substances

  • Anti-Bacterial Agents
  • Urea
  • Stk1 protein, Streptococcus agalactiae
  • Protein Serine-Threonine Kinases