Discovery and Evaluation of Thiazinoquinones as Anti-Protozoal Agents

  title={Discovery and Evaluation of Thiazinoquinones as Anti-Protozoal Agents},
  author={Cary F. C. Lam and A. Norrie Pearce and Shen H. Tan and M Kaiser and Brent R Copp},
  booktitle={Marine drugs},
Pure compound screening has identified the dioxothiazino-quinoline-quinone ascidian metabolite ascidiathiazone A (2) to be a moderate growth inhibitor of Trypanosoma brucei rhodesiense (IC₅₀ 3.1 μM) and Plasmodium falciparum (K1 dual drug resistant strain) (IC₅₀ 3.3 μM) while exhibiting low levels of cytotoxicity (L6, IC₅₀ 167 μM). A series of C-7 amide and Δ²(³) analogues were prepared that explored the influence of lipophilicity and oxidation state on observed anti-protozoal activity and… CONTINUE READING


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