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Updated: Sep 20, 2026

Synthesis and Assay of Vibrio Quorum Sensing Inhibitors
Published on: May 31, 2024
8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone, a non-competitive inhibitor of trypanothione reductase
Carlos L Zani1, Alan H Fairlamb
1Laboratório de Química de Produtos Naturais, Centro de Pesquisas Ren Rachou, Fiocruz, Belo Horizonte, MG, 30190-002, Brasil. zani@cpqrr.fiocruz.br
Abstract:
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.
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