Author(s): Ballard TE, Wang X, Olekhnovich I, Koerner T, Seymour C,
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Abstract A library composed of nitazoxanide-based analogues was synthesized and assayed for increased antibacterial efficacy against the pyruvate-ferredoxin oxidoreductase (PFOR) using microorganisms Helicobacter pylori, Campylobacter jejuni and Clostridium difficile. Derivatives were found to recapitulate and improve activity against these organisms and select analogues were tested for their ability to disrupt the PFOR enzyme directly. The library was also screened for activity against staphylococci and resulted in the identification of analogues capable of inhibiting both staphylococci and all PFOR organisms at low micromolar minimum inhibitory concentrations with low toxicity to human foreskin cells. Copyright © 2011 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.
This article was published in ChemMedChem
and referenced in Journal of Developing Drugs