Identification of arylsulfonamides as ExoU inhibitors

[Display omitted] 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 activ...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2014-08, Vol.24 (16), p.3823-3825
Main Authors: Kim, Doran, Baek, Jihae, Song, Jiho, Byeon, Hyeyoung, Min, Hyeyoung, Min, Kyung Hoon
Format: Article
Language:English
Subjects:
Bacterial Proteins - antagonists & inhibitors
Cell Survival - drug effects
Dose-Response Relationship, Drug
ExoU
HEK293 Cells
Humans
Molecular Structure
Pseudomonas aeruginosa
Small molecule
Structure-Activity Relationship
Sulfonamides
Sulfonamides - chemical synthesis
Sulfonamides - chemistry
Sulfonamides - pharmacology
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Summary:[Display omitted] 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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2014.06.064