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Literature summary for 1.8.1.12 extracted from

  • Stump, B.; Kaiser, M.; Brun, R.; Krauth-Siegel, R.L.; Diederich, F.
    Betraying the parasites redox system: diaryl sulfide-based inhibitors of trypanothione reductase: subversive substrates and antitrypanosomal properties (2007), ChemMedChem, 2, 1708-1712.
    View publication on PubMed
Search for more literature for 1.8.1.12

Application

Application Comment Organism
medicine promising trypanothione reductase inhibitors Trypanosoma brucei rhodesiense

Inhibitors

Inhibitors Comment Organism Structure
3-([2-[(4-bromophenyl)sulfanyl]-5-chlorophenyl]amino)-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide cationic diaryl sulphide-based inhibitor, 99% growth inhibition Trypanosoma brucei rhodesiense
3-([2-[(4-bromophenyl)sulfanyl]-5-chlorophenyl]amino)-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride cationic diaryl sulphide-based inhibitor Trypanosoma brucei rhodesiense
3-([5-chloro-2-[(4-chlorophenyl)sulfanyl]phenyl]amino)-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide cationic diaryl sulphide-based inhibitor, 99% growth inhibition Trypanosoma brucei rhodesiense
3-([5-chloro-2-[(4-chlorophenyl)sulfanyl]phenyl]amino)-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride cationic diaryl sulphide-based inhibitor Trypanosoma brucei rhodesiense
3-[(5-chloro-2-[[4-(trifluoromethyl)phenyl]sulfanyl]phenyl)amino]-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide cationic diaryl sulphide-based inhibitor, 99% growth inhibition Trypanosoma brucei rhodesiense
3-[(5-chloro-2-[[4-(trifluoromethyl)phenyl]sulfanyl]phenyl)amino]-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride cationic diaryl sulphide-based inhibitor, 38% growth inhibition Trypanosoma brucei rhodesiense
3-[[5-chloro-2-(phenylsulfanyl)phenyl]amino]-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide cationic diaryl sulphide-based inhibitor, 99% growth inhibition Trypanosoma brucei rhodesiense
3-[[5-chloro-2-(phenylsulfanyl)phenyl]amino]-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride cationic diaryl sulphide-based inhibitor, 0% growth inhibition Trypanosoma brucei rhodesiense
chinifur inhibits trypanothione reductase and acts as subversive substrate Trypanosoma brucei rhodesiense
nifurtimox weak inhibitor of trypanothione reductase Trypanosoma brucei rhodesiense

Organism

Organism UniProt Comment Textmining
Trypanosoma brucei rhodesiense
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
trypanothione + 5,5'-dithiobis-(2-nitrobenzoic acid)
-
 Trypanosoma brucei rhodesiense trypanothione disulfide + thionitrobenzoate
-
 ?
trypanothione + NADP+
-
 Trypanosoma brucei rhodesiense trypanothione disulfide + NADPH + H+
-
 ?

Synonyms

Synonyms Comment Organism
trypanothione reductase TR Trypanosoma brucei rhodesiense

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.006
-
 3-[(5-chloro-2-[[4-(trifluoromethyl)phenyl]sulfanyl]phenyl)amino]-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride
-
 Trypanosoma brucei rhodesiense
0.007
-
 3-([2-[(4-bromophenyl)sulfanyl]-5-chlorophenyl]amino)-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide
-
 Trypanosoma brucei rhodesiense
0.007
-
 3-([5-chloro-2-[(4-chlorophenyl)sulfanyl]phenyl]amino)-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide
-
 Trypanosoma brucei rhodesiense
0.008
-
 3-([2-[(4-bromophenyl)sulfanyl]-5-chlorophenyl]amino)-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride
-
 Trypanosoma brucei rhodesiense
0.009
-
 3-[[5-chloro-2-(phenylsulfanyl)phenyl]amino]-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide
-
 Trypanosoma brucei rhodesiense
0.009
-
 3-[[5-chloro-2-(phenylsulfanyl)phenyl]amino]-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride
-
 Trypanosoma brucei rhodesiense
0.01
-
 3-([5-chloro-2-[(4-chlorophenyl)sulfanyl]phenyl]amino)-N-(3,4-dichlorobenzyl)-N,N-dimethylpropan-1-aminium chloride
-
 Trypanosoma brucei rhodesiense
0.02
-
 3-[(5-chloro-2-[[4-(trifluoromethyl)phenyl]sulfanyl]phenyl)amino]-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide
-
 Trypanosoma brucei rhodesiense

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000059
-
-
 Trypanosoma brucei rhodesiense 3-[[5-chloro-2-(phenylsulfanyl)phenyl]amino]-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide
0.000068
-
-
 Trypanosoma brucei rhodesiense 3-([2-[(4-bromophenyl)sulfanyl]-5-chlorophenyl]amino)-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide
0.000077
-
-
 Trypanosoma brucei rhodesiense 3-([5-chloro-2-[(4-chlorophenyl)sulfanyl]phenyl]amino)-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide
0.000102
-
-
 Trypanosoma brucei rhodesiense 3-[(5-chloro-2-[[4-(trifluoromethyl)phenyl]sulfanyl]phenyl)amino]-N,N-dimethyl-N-[(5-nitrofuran-2-yl)methyl]propan-1-aminium bromide