Add time:09/04/2019         Source:sciencedirect.com

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 (cas 121-66-4) counterparts, demonstrating that head group modification is a viable route for the synthesis of NTZ-related antibacterial analogues.

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