Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 20, Issue 12, Pages 3537-3539Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2010.04.126
Keywords
Nitazoxanide; Antibacterial; Small-molecule drug target; Pyruvate:ferredoxin oxidoreductase; Helicobacter pylori; Campylobacter jejuni; Clostridium difficile
Categories
Funding
- National Institute of Allergy and Infectious Diseases [AI075520]
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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. (C) 2010 Elsevier Ltd. All rights reserved.
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