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Literature summary for 1.8.1.12 extracted from

  • Arias, D.G.; Herrera, F.E.; Garay, A.S.; Rodrigues, D.; Forastieri, P.S.; Luna, L.E.; Buergi, M.D.; Prieto, C.; Iglesias, A.A.; Cravero, R.M.; Guerrero, S.A.
    Rational design of nitrofuran derivatives Synthesis and valuation as inhibitors of Trypanosoma cruzi trypanothione reductase (2017), Eur. J. Med. Chem., 125, 1088-1097 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
5-nitro-furan-2-carboxylic acid (3-dimethylamino-propyl)-amide reversible uncompetitive inhibition regarding substrate trypanothione disulfide, IC50 value for Trypanooma cruzi growth inhibition 0.0019 microM, EC50 value for toxicity against HeLa cells 0.074 microM Trypanosoma cruzi
5-nitrofuran-2-carboxylic acid benzylamide reversible uncompetitive inhibition regarding substrate trypanothione disulfide, IC50 value for Trypanooma cruzi growth inhibition 0.0015 microM, EC50 value for toxicity against HeLa cells 0.123 microM Trypanosoma cruzi
5-nitrofuran-2-carboxylic acid dibenzylamide reversible uncompetitive inhibition regarding substrate trypanothione disulfide, IC50 value for Trypanooma cruzi growth inhibition 0.0001 microM, EC50 value for toxicity against HeLa cells 0.078 microM Trypanosoma cruzi
nifurtimox
-
Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi V5AJG2
-
-
Trypanosoma cruzi Dm28c V5AJG2
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione disulfide + NADPH + H+
-
Trypanosoma cruzi trypanothione + NADP+
-
?
trypanothione disulfide + NADPH + H+
-
Trypanosoma cruzi Dm28c trypanothione + NADP+
-
?

Synonyms

Synonyms Comment Organism
TCDM_11669
-
Trypanosoma cruzi

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Trypanosoma cruzi

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.061
-
5-nitrofuran-2-carboxylic acid benzylamide pH 7.5, 30°C Trypanosoma cruzi
0.068
-
5-nitrofuran-2-carboxylic acid dibenzylamide pH 7.5, 30°C Trypanosoma cruzi
0.118
-
5-nitro-furan-2-carboxylic acid (3-dimethylamino-propyl)-amide pH 7.5, 30°C Trypanosoma cruzi
0.245
-
nifurtimox pH 7.5, 30°C Trypanosoma cruzi