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Please use this identifier to cite or link to this item: http://hdl.handle.net/1807/8103

Title: 8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone, a Non-competitive Inhibitor of Trypanothione Reductase
Authors: Zani, Carlos L.
Fairlamb, Alan H.
Keywords: trypanothione reductase - Trypanosoma cruzi - Leishmania - enzyme inhibitors - naphthoquinone
Issue Date: 31-Dec-2003
Publisher: Fundação Oswaldo Cruz, Fiocruz
Citation: Memórias do Instituto Oswaldo Cruz (ISSN: 1678-8060) Vol 98 Num 4
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 μM, respectively. When tested against human glutathione reductase, this compound did not display any significant inhibition at 100 μM, indicating a good selectivity against the parasite enzyme.
URI: http://hdl.handle.net/1807/8103
Other Identifiers: http://www.bioline.org.br/abstract?id=oc03122
Rights: Copyright 2003 - Instituto Oswaldo Cruz - Fiocruz
Appears in Collections:Bioline International Legacy Collection

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