8-Methoxy-naphtho[2,3-b]thiophen-4,9-quinone, a non-competitive inhibitor of trypanothione reductase
Mem. Inst. Oswaldo Cruz
;
98(4): 565-568, June 2003. ilus, tab, graf
Article
in English
| LILACS
| ID: lil-344256
RESUMO
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 æM, respectively. When tested against human glutathione reductase, this compound did not display any significant inhibition at 100 æM, indicating a good selectivity against the parasite enzyme
Full text:
Available
Index:
LILACS (Americas)
Main subject:
Thiophenes
/
Trypanosoma cruzi
/
Naphthoquinones
/
Enzyme Inhibitors
/
NADP
Type of study:
Prognostic study
Limits:
Animals
/
Humans
Language:
English
Journal:
Mem. Inst. Oswaldo Cruz
Journal subject:
Tropical Medicine
/
Parasitology
Year:
2003
Type:
Article
Affiliation country:
Brazil
/
United kingdom
Institution/Affiliation country:
Fiocruz/BR
/
University of Dundee/GB
Similar
MEDLINE
...
LILACS
LIS