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Literature summary extracted from

  • Cavalli, A.; Lizzi, F.; Bongarzone, S.; Brun, R.; Luise Krauth-Siegel, R.; Bolognesi, M.L.
    Privileged structure-guided synthesis of quinazoline derivatives as inhibitors of trypanothione reductase (2009), Bioorg. Med. Chem. Lett., 19, 3031-3035.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.8.1.12 2-(4-[4-amino-6,7-bis[2-(dimethylamino)ethoxy]quinazolin-2-yl]piperazin-1-yl)naphthalene-1,4-dione non-competitive inhibition, 79% inhibition at 0.05 mM Trypanosoma cruzi
1.8.1.12 2-[4-(1H-indol-3-ylacetyl)piperazin-1-yl]-6,7-dimethoxyquinazolin-4-amine 23% inhibition at 0.1 mM Trypanosoma cruzi
1.8.1.12 2-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-5-methoxycyclohexa-2,5-diene-1,4-dione non-competitive inhibition, 75% inhibition at 0.1 mM Trypanosoma cruzi
1.8.1.12 2-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]naphthalene-1,4-dione mixed-type inhibition, 57% inhibition at 0.1 mM Trypanosoma cruzi
1.8.1.12 4,4'-bis(4-benzyloxy-3-methoxybenzimidoylamino)di-cyclohexylmethane 97% inhibition at 0.1 mM, in the presence of 0.1 mM trypanothione disulfide Trypanosoma cruzi
1.8.1.12 6,7-bis[2-(dimethylamino)ethoxy]-2-[4-(1H-indol-3-ylacetyl)piperazin-1-yl]quinazolin-4-amine 44% inhibition at 0.05 mM Trypanosoma cruzi
1.8.1.12 6,7-dimethoxy-2-[4-[(3R)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]piperazin-1-yl]quinazolin-4-amine complete inhibition at 0.1 mM Trypanosoma cruzi
1.8.1.12 6,7-dimethoxy-2-[4-[(3S)-1,2,3,4-tetrahydroisoquinolin-3-ylcarbonyl]piperazin-1-yl]quinazolin-4-amine complete inhibition at 0.1 mM Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
1.8.1.12 Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
1.8.1.12 EC 1.6.4.8 formerly Trypanosoma cruzi
1.8.1.12 trypanothione reductase
-
 Trypanosoma cruzi

Cofactor

EC Number Cofactor Comment Organism Structure
1.8.1.12 NADPH
-
 Trypanosoma cruzi

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.8.1.12 0.002
-
 4,4'-bis(4-benzyloxy-3-methoxybenzimidoylamino)di-cyclohexylmethane
-
 Trypanosoma cruzi
1.8.1.12 0.0075
-
 2-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]naphthalene-1,4-dione
-
 Trypanosoma cruzi
1.8.1.12 0.011
-
 2-(4-[4-amino-6,7-bis[2-(dimethylamino)ethoxy]quinazolin-2-yl]piperazin-1-yl)naphthalene-1,4-dione
-
 Trypanosoma cruzi
1.8.1.12 0.032
-
 2-[4-(4-amino-6,7-dimethoxyquinazolin-2-yl)piperazin-1-yl]-5-methoxycyclohexa-2,5-diene-1,4-dione
-
 Trypanosoma cruzi