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(E)-3-(4-fluorophenyl)-N-[4-(1-hydroxy-6-nitrobenzimidazol-2-yl)phenyl]prop-2-enamide

Drug details:
Molecular formula: C22H15FN4O4

Classification: Phenylbenzimidazoles; Benzimidazoles; Organoheterocyclic compounds; Organic compounds;
Chemical structure:
Depiction based on curated SMILES HO N _ O O + N N O N H F

Evidence for compound's anti-virulence activity:

Pseudomonas
Related VF: TTSS (Type III secretion system)
Target: ExsA
Drug effect: Inhibits DNA binding by interacting specifically with the DNA-binding domain of ExsA and its homologs AscA, LscA, LcrF, ExsAvp (from Vibrio parahaemolyticus).
Max phase: Preclinical (in vitro)
Publication:
Marsden AE, et al., 2016. Inhibition of Pseudomonas aeruginosa ExsA DNA-Binding Activity by N-Hydroxybenzimidazoles. Antimicrob Agents Chemother 60(2):766-76.

Yersinia
Related VF: TTSS (Type III secretion system)
Target: VirF/LcrF
Drug effect: Targets the conserved DNA-binding domain of LcrF.
Max phase: Preclinical (in vitro)
Publication:
Kim OK, et al., 2009. N-hydroxybenzimidazole inhibitors of the transcription factor LcrF in Yersinia: novel antivirulence agents. J Med Chem 52(18):5626-34.

Yersinia
Related VF: TTSS (Type III secretion system)
Target: VirF/LcrF
Drug effect: Targets the conserved DNA-binding domain of LcrF.
Max phase: Preclinical (in vivo)
Publication:
Garrity-Ryan LK, et al., 2010. Small molecule inhibitors of LcrF, a Yersinia pseudotuberculosis transcription factor, attenuate virulence and limit infection in a murine pneumonia model. Infect Immun 78(11):4683-90.








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