Discovery of new Gram-negative antivirulence drugs: structure and properties of novel E. coli WaaC inhibitors.

Bioorg. Med. Chem. Lett.2008 Jul 15;18(14):4022-6. Epub 2008 Jun 05

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Heptosyltransferases such as WaaC represent promising and attractive targets for the discovery of new Gram-negative antibacterial drugs based on antivirulence mechanisms. We report herein our approach to the identification of the first micromolar inhibitors of WaaC and the preliminary SAR generated from this family of 2-aryl-5-methyl-4-(5-aryl-furan-2-yl-methylene)-2,4-dihydro-pyrazol-3-ones identified by virtual screening.

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Discovery of new Gram-negative antivirulence drugs: structure and properties of novel E. coli WaaC inhibitors.

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