Author(s): Ballard TE, Wang X, Olekhnovich I, Koerner T, Seymour C,
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Abstract Head group analogues of the antibacterial and antiparasitic drug nitazoxanide (NTZ) are presented. A library of 39 analogues was synthesized and assayed for their ability to suppress growth of Helicobacter pylori, Campylobacter jejuni, Clostridium difficile and inhibit NTZ target pyruvate:ferredoxin oxidoreductase (PFOR). Two head groups assayed recapitulated NTZ activity and possessed improved activity over their 2-amino-5-nitrothiazole counterparts, demonstrating that head group modification is a viable route for the synthesis of NTZ-related antibacterial analogues. Copyright 2010 Elsevier Ltd. All rights reserved.
This article was published in Bioorg Med Chem Lett
and referenced in Journal of Developing Drugs