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]
- 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 YesAntagonistInhibitorDetails