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

@article{Ballard2010BiologicalAO,
  title={Biological activity of modified and exchanged 2-amino-5-nitrothiazole amide analogues of nitazoxanide.},
  author={T Eric Ballard and Xia Wang and Igor N. Olekhnovich and Taylor Koerner and Craig R Seymour and Paul S. Hoffman and Timothy L. Macdonald},
  journal={Bioorganic & medicinal chemistry letters},
  year={2010},
  volume={20 12},
  pages={3537-9}
}
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… CONTINUE READING