title: Evaluating 5-Nitrothiazoles as Trypanocidal Agents.
abstract: The growth-inhibitory properties of a 5-nitrothiazole series were evaluated against Trypanosoma brucei. A subset of related compounds displayed the greatest potency toward the parasite while exhibiting little cytotoxic effect on mammalian cells, with this antiparasitic activity dependent on expression of a type I nitroreductase by the trypanosome. We conclude that the 5-nitrothiazole class of nitroheterocyclic drugs may represent a new lead in the treatment of human African trypanosomiasis.
authors.affiliation: School of Biological and Chemical Sciences, Queen Mary University of London, London, United Kingdom.
authors.forename: Ivan P
authors.initials: IP
authors.lastname: O'Shea
authors.affiliation: School of Biological and Chemical Sciences, Queen Mary University of London, London, United Kingdom.
authors.forename: Mohammed
authors.initials: M
authors.lastname: Shahed
authors.affiliation: Laboratory of Antioxidants, Institute of Nutrition and Food Technology, University of Chile, Santiago, Chile.
authors.forename: Benjamín
authors.initials: B
authors.lastname: Aguilera-Venegas
authors.affiliation: School of Biological and Chemical Sciences, Queen Mary University of London, London, United Kingdom s.r.wilkinson@qmul.ac.uk.
authors.forename: Shane R
authors.initials: SR
authors.lastname: Wilkinson
mesh_terms: D000818:Animals; D002460:Cell Line; D004353:Drug Evaluation, Preclinical / Q000379:methods; D020128:Inhibitory Concentration 50; D008322:Mammals; D009601:Nitroreductases / Q000235:genetics / Q000378:metabolism; D013329:Structure-Activity Relationship; D013844:Thiazoles / Q000737:chemistry* / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000737:chemistry* / Q000494:pharmacology*; D014346:Trypanosoma brucei brucei / Q000187:drug effects* / Q000235:genetics / Q000378:metabolism
chemical_list: C581042:5-nitrothiazole; D013844:Thiazoles; D014344:Trypanocidal Agents; D009601:Nitroreductases