Identification of arylsulfonamides as ExoU inhibitors

Bioorg Med Chem Lett. 2014 Aug 15;24(16):3823-5. doi: 10.1016/j.bmcl.2014.06.064. Epub 2014 Jun 27.

Abstract

ExoU is a potent virulence factor of Pseudomonas aeruginosa and is considered a potential therapeutic target. In order to discover novel ExoU inhibitors, we screened an in-house chemical library utilizing a yeast-based screening system. Some sulfonamides displayed significant activity without nonspecific cytotoxicity. We describe a series of sulfonamides as novel ExoU inhibitors, along with a brief structure-activity relationship.

Keywords: ExoU; Pseudomonas aeruginosa; Small molecule; Sulfonamides.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Bacterial Proteins / antagonists & inhibitors*
  • Cell Survival / drug effects
  • Dose-Response Relationship, Drug
  • HEK293 Cells
  • Humans
  • Molecular Structure
  • Structure-Activity Relationship
  • Sulfonamides / chemical synthesis
  • Sulfonamides / chemistry
  • Sulfonamides / pharmacology*

Substances

  • Bacterial Proteins
  • Sulfonamides
  • pseudomonas exoprotein A protein, Pseudomonas aeruginosa