Table 3

Antivirulence compounds

Antivirulence strategiesCompound/name in studyTarget/mode of actionIndication(s)Reference(s)
ToxinsPer–6–(3–aminopropylthio)–β–cyclodextrinPA heptamer pore/blocks toxin bindingAnthrax 440
2(R)-2[(4-Fluoro-3-methyl-phenyl)sulfonylamino]-N-hydroxy-2-(tetrahydro-2H-pyran-4-yl)acetamideLF subunit/inhibited by protease activityAnthrax 441
CisplatinLF subunit/inhibited by degradation of MAPKKAnthrax 442
Synsorb-PkGb3/blocks toxin bindingEnterohemorrhagic E. coli and hemolytic-uremic syndrome 443, 444
Adhesion and colonizationBicyclic 2-pyridones (pilicides)PapD/prevents pilus assemblyUrinary tract infection; replacement of conventional antibiotics 445
VirstatinToxT/inhibitor of regulator of pilus assemblyReplacement of conventional antibiotics 446
Bacterial secretory systemAcylated hydrazones of salicylaldehydesYop/inhibition of type III secretion systems Chlamydia and Shigella sp. infections; replacement of conventional antibiotics 447, 448
2-Imino-5-arylidene thiazolidinoneSip/inhibition of type III secretion systems Salmonella, Pseudomonas, and Yersinia sp. infections; replacement of conventional antibiotics 449
DiarylacrylonitrileInhibition of sortase AActivity in vitro against S. aureus 450
Cell-to-cell signalingFuranones (C-30)AHLs/inhibition of quorum sensing Pseudomonas infections; replacement of conventional antibiotics 451, 452, 453
ThiophenonesIcaC, LrgB/inhibition of quorum-sensing Staphylococcus epidermidis infections
Substrate analogs 3/oxo C12 D10LasR/all competition, inhibition of quorum sensing Pseudomonas infections; replacement of conventional antibiotics 454
Substrate analogs/C4LuxR/TraR antagonist, inhibition of quorum sensing Vibrio fischeri infections; replacement of conventional antibiotics 432, 454
7-FluoroindoleInhibition of quorum sensing Pseudomonas infections; replacement of conventional antibiotics 455
Catechins (galloyl group)Lux system/inhibition of quorum sensing Vibrio harveyi and Eikenella corrodens infections; replacement of conventional antibiotics 456, 457
TomatidineAgr system inhibitor S. aureus infections; potentiator of the action of aminoglycoside antimicrobials 403
26%HACC-loaded PMMA (chitosan derivative) icaAD-icaR/inhibition of biofilm formation, including antibiotic-resistant strainsImplant infections and osteomyelitis caused by methicillin-resistant S. aureus 402
Salicilate marA-fimB regulator/inhibition of biofilm formation In vitro activity against E. coli 458
LED 209QscE/inhibition of quorum-sensingPostexposure to the pathogen; replacement of conventional antibiotics 458
Iron metabolismAcyladenylate derivatesMbtA in M. tuberculosis, YbtE in Y. pestis, inhibition of aryl acyl adenylating enzymes In vitro activity against M. tuberculosis and Y. pestis 459, 460
Piridine derivative/HTS 85KBasE/nonnucleoside inhibitor A. baumannii infections 294
Virulence factors involved in host immune responseI-A09mPTPB inhibitor/resistance to stress oxidativePrevention of M. tuberculosis growth in host cells 461
Sulfamoyl d-AlaDltA/protection against cationic effectors of the innate immunity In vitro activity against B. subtilis strains that are more sensitive to vancomycin 462
RND efflux pump inhibitors1-(1-Naphthylmethyl)-piperazine, phenyl-arginine-β-naphthylamideRND efflux pumps, cholera toxin factor, toxin-coregulated pilus/increased susceptibility and inhibition of production of virulence factors In vitro activity against V. cholerae 404
Trifluoromethyl ketones (12 compounds)RND efflux pumps and quorum-sensing inhibitor/regulation of cell functions (virulence, biofilms, and motility) In vitro activity against C. violaceum 026 and E. coli 401