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• W2083967568 abstract "New antimicrobials are needed because of the emergence of organisms that are resistant to available antimicrobials. The purpose of this study was to evaluate a high-throughput screening approach to identify antibacterials against two common disease-causing bacteria, and to determine the frequency, novelty, and potency of compounds with antibacterial activity.A high-throughput, turbidometric assay of bacterial growth in a 96-well plate format was used to screen a diverse collection of 150,000 small molecules for antibacterial activity against E. coli and P. aeruginosa. The statistical Z'-factor for the assay was > or = 0.7.Screening for inhibition of E. coli growth gave a 'hit' rate (> 60% inhibition at 12.5 microM) of 0.025%, which was more than 5-fold reduced for P. aeruginosa. The most potent antibacterials (EC50 < 0.5 microM) were of the nitrofuran class followed by naphthalimide, salicylanilide, bipyridinium and quinoazolinediamine chemical classes. Screening of > 250 analogs of the most potent antibacterial classes established structure-activity data sets.Our results validate and demonstrate the utility of a growth-based phenotype screen for rapid identification of small-molecule antibacterials. The favourable efficacy and structure-activity data for several of the antibacterial classes suggests their potential development for clinical use." @default.
• W2083967568 created "2016-06-24" @default.
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• W2083967568 date "2006-11-01" @default.
• W2083967568 modified "2023-09-27" @default.
• W2083967568 title "Small molecules with antimicrobial activity against <i>E. coli</i> and <i>P. aeruginosa</i> identified by high-throughput screening" @default.
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• W2083967568 doi "https://doi.org/10.1038/sj.bjp.0706873" @default.
• W2083967568 hasPubMedCentralId "https://www.ncbi.nlm.nih.gov/pmc/articles/2014677" @default.
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