Biological activity of modified and exchanged 2-amino-5-nitrothiazole amide analogues of nitazoxanide.

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Ballard TE, Wang X, Olekhnovich I, Koerner T, Seymour C, Hoffman PS, Macdonald TL

Biological activity of modified and exchanged 2-amino-5-nitrothiazole amide analogues of nitazoxanide.

Bioorg Med Chem Lett. 2010 Jun 15;20(12):3537-9. doi: 10.1016/j.bmcl.2010.04.126. Epub 2010 May 18.

PubMed ID

20488706 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Nitazoxanide	Pyruvate-flavodoxin oxidoreductase	Protein	Desulfovibrio africanus	Yes	Antagonist Inhibitor	Details