8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone, a non-competitive inhibitor of trypanothione reductase.

The enzyme trypanothione reductase is a recognised drug target in trypanosomatids and has been used in the search of new compounds with potential activity against diseases such as leishmaniasis, Chagas disease and African trypanosomiasis. 8-Methoxy-naphtho [2,3-b] thiophen-4,9-quinone was selected in a screening of natural and synthetic compounds using an in vitro assay with the recombinant enzyme from Trypanosoma cruzi. Its mode of inhibition fits a non-competitive model with respect to the substrate (trypanothione) and to the co-factor (NADPH), with Ki-values of 5 and 3.6 M, respectively. When tested against human glutathione reductase, this compound did not display any significant inhibition at 100 M, indicating a good selectivity against the parasite enzyme.
AuthorsCarlos L Zani, Alan H Fairlamb
JournalMemoĢrias do Instituto Oswaldo Cruz (Mem Inst Oswaldo Cruz) Vol. 98 Issue 4 Pg. 565-8 (Jun 2003) ISSN: 0074-0276 [Print] Brazil
PMID12937775 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)
Chemical References
  • 8-methoxy-naphtho(2,3-b)thiophen-4,9-quinone
  • Enzyme Inhibitors
  • Quinones
  • NADP
  • NADH, NADPH Oxidoreductases
  • trypanothione reductase
  • Animals
  • Enzyme Inhibitors (pharmacology)
  • Humans
  • Inhibitory Concentration 50
  • NADH, NADPH Oxidoreductases (antagonists & inhibitors, metabolism)
  • NADP (antagonists & inhibitors, metabolism)
  • Parasitic Sensitivity Tests
  • Quinones (pharmacology)
  • Trypanosoma cruzi (drug effects, enzymology)

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