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Literature summary for 1.8.1.12 extracted from

  • Galarreta, B.C.; Sifuentes, R.; Carrillo, A.K.; Sanchez, L.; Amado, M.d.e.l.R.; Maruenda, H.
    The use of natural product scaffolds as leads in the search for trypanothione reductase inhibitors (2008), Bioorg. Med. Chem., 16, 6689-6695.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1,3-bis[3-(dimethylamino)propyl]-1,5-dihydro-2H-pyrimido[4,5-beta][1,4]benzothiazine-2,4(3H)-dione 11% growth inhibition, no inhibition of glutathione reductase Leishmania amazonensis
1,3-bis[3-(dimethylamino)propyl]-1,5-dihydro-2H-pyrimido[4,5-beta][1,4]benzothiazine-2,4(3H)-dione no inhibition of glutathione reductase Trypanosoma cruzi
aspidospermine 11% growth inhibition, no inhibition of glutathione reductase Leishmania amazonensis
aspidospermine no inhibition of glutathione reductase Trypanosoma cruzi
connesine 97% growth inhibition Leishmania amazonensis
N,N-dimethyl-N-[3-(7-methoxy-1-methyl-3,4-dihydro-9H-beta-carbolin-9-yl)propyl]amine 57% growth inhibition, no inhibition of glutathione reductase, twenty-three heterocyclic compounds are evaluated for their potential as trypanothione reductase inhibitors Leishmania amazonensis
N,N-dimethyl-N-[3-(7-methoxy-1-methyl-3,4-dihydro-9H-beta-carbolin-9-yl)propyl]amine no inhibition of glutathione reductase, twenty-three heterocyclic compounds are evaluated for their potential as trypanothione reductase inhibitors Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Leishmania amazonensis
-
-
-
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione + 5,5'-dithiobis-(2-nitrobenzoic acid) inhibitors are tested using the recombinant enzyme Trypanosoma cruzi trypanothione disulfide + thionitrobenzoate
-
?
trypanothione + 5,5'-dithiobis-(2-nitrobenzoic acid) inhibitors are tested using the recombinant enzyme Leishmania amazonensis trypanothione disulfide + thionitrobenzoate
-
?
trypanothione + NADP+
-
Trypanosoma cruzi trypanothione disulfide + NADPH + H+
-
?
trypanothione + NADP+
-
Leishmania amazonensis trypanothione disulfide + NADPH + H+
-
?

Synonyms

Synonyms Comment Organism
trypanothione reductase TR Trypanosoma cruzi
trypanothione reductase TR Leishmania amazonensis

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.0269
-
1,3-bis[3-(dimethylamino)propyl]-1,5-dihydro-2H-pyrimido[4,5-beta][1,4]benzothiazine-2,4(3H)-dione
-
Trypanosoma cruzi
0.035
-
N,N-dimethyl-N-[3-(7-methoxy-1-methyl-3,4-dihydro-9H-beta-carbolin-9-yl)propyl]amine
-
Trypanosoma cruzi
0.0646
-
aspidospermine
-
Trypanosoma cruzi

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0904
-
-
Leishmania amazonensis aspidospermine