6.3.1.9: trypanothione synthase
This is an abbreviated version!
For detailed information about trypanothione synthase, go to the full flat file.
Word Map on EC 6.3.1.9
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6.3.1.9
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trypanosoma
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leishmania
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trypanosomatids
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brucei
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cruzi
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fasciculata
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crithidia
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n1,n8-bisglutathionylspermidine
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chagas
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infantum
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tryparedoxine
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antileishmanial
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parasite-specific
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kinetoplastida
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antitrypanosomal
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drug development
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synthesis
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pharmacology
- 6.3.1.9
- trypanosoma
- leishmania
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trypanosomatids
- brucei
- cruzi
- fasciculata
- crithidia
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n1,n8-bisglutathionylspermidine
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chagas
- infantum
-
tryparedoxine
-
antileishmanial
-
parasite-specific
- kinetoplastida
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antitrypanosomal
- drug development
- synthesis
- pharmacology
Reaction
Synonyms
Cf-TS, GenBank AF006615-derived protein GI 3004644, LdTryS, LiTRYS, Synthetase, trypanothione, Synthetase, trypanothione (Crithidia fasciculata strain HS6 gene Cf-TS), T(SH)2 synthetase, TbTryS, TcTryS, TRS, trypanothione synthase, Trypanothione synthetase, Trypanothione synthetase (Crithidia fasciculata strain HS6 gene Cf-TS), trypanothione synthetase-amidase, TryS, TSA, TSH synthetase, tyrS
ECTree
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Inhibitors
Inhibitors on EC 6.3.1.9 - trypanothione synthase
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(Z)-8-(2-(2,4-dihydroxybenzylidene)hydrazinyl)-7-(2-hydroxy-3-phenoxy propyl)-1,3-dimethyl-1H-purine-2,6(3H,7H)-dione
88.5% activity remaining
1,3,5-trimethyl-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-1H-pyrazole-4-sulfonamide
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1,4,7-trioxo-1lambda5,4lambda5,7lambda5-benzo[1,2-c:3,4-c':5,6-c'']tris[1,2,5]oxadiazole
64.4% activity remaining
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
83.5% activity remaining
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
1-(3-(1-isobutyl-1H-pyrazol-4-yl)-1H-indazol-1-yl)-3,3-dimethylbutan-2-one
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1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(3,4-dimethoxybenzoyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
1-[3-(3-fluorophenyl)-1H-indazol-1-yl]-3,3-dimethylbutan-2-one
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i.e. DDD85811, inhibits growth of bloodstream Trypanosoma brucei in vitro
1-[5-(3-chloro-4-methylphenyl)-2H-tetrazol-2-yl]-3,3-dimethylbutan-2-one
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2,4-dimethyl-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]-1,3-thiazole-5-sulfonamide
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2,4-dimethyl-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]thiophene-3-sulfonamide
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2,6-dichloro-N-[(3-phenyl-1,2,4-oxadiazol-5-yl)methyl]benzenesulfonamide
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2,6-dimethoxy-N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]benzenesulfonamide
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2-(3-(3-fluorophenyl)-1H-indazol-1-yl)-N-(2-(4-methylpiperazin-1-yl)ethyl)acetamide
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2-(3-(3-fluorophenyl)-1H-indazol-1-yl)-N-(3-(4-methylpiperazin-1-yl)propyl)acetamide
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2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide
2-methyl-N-((5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl)propane-2-sulfonamide
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2-[3-(3-fluorophenyl)-1H-indazol-1-yl]-1-(piperidin-1-yl)ethanone
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i.e. DDD86243, inhibits growth of bloodstream Trypanosoma brucei in vitro. Exposure to DDD86243 at 2 x EC50 for 72 h decreases intracellular trypanothione levels to less than 10% of wild type, with a corresponding 5fold increase in the precursor metabolite, glutathione
3,3-dimethyl-1-(3-(1-methyl-1H-indol-4-yl)-1H-indazol-1-yl)butan-2-one
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3,3-dimethyl-1-[5-[3-(trifluoromethyl)phenyl]-2H-tetrazol-2-yl]butan-2-one
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3,3-dimethyl-1-[5-[4-(trifluoromethyl)phenyl]-2H-tetrazol-2-yl]butan-2-one
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4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-1-(6-methoxy-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1-(6-methyl-1,3-benzothiazol-2-yl)-1,5-dihydro-2H-pyrrol-2-one
83.9% activity remaining
4-methoxy-N-[[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]benzenesulfonamide
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6-fluoro-3-oxo-4,5-didehydro-2,1,3lambda5-benzoxadiazole
84.1% activity remaining
DL-(S,R)-buthionine sulfoximine
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DL-(S,R)-BSO, a multitarget inhibitor of trypanothione synthesis, in vivo effects on nonthiol-supplied epimastigote cells, on Cys-supplied epimastigote cells, and on GSH-supplied epimastigote cells, overview. Inhibition of gamma-glutamylcysteine synthetase and trypanothione synthetase. Wild-type Trypanosoma brucei cells are not restored by supplementing with 0.08 mM GSH. The the L-(S,R)-BSO stereoisomer is more potent that the the D-(S,R)-BSO. Inhibitor docking analysis, binding structure
N,N-dibenzyl-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N,N-diethyl-2-(3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl)acetamide
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N-(1-phenylethyl)-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-(2-(dimethylamino)ethyl)-2-(3-(3-fluorophenyl)-1H-indazol-1-yl)acetamide
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N-(2-methoxyethyl)-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-(2-phenylethyl)-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-(3-(1H-imidazol-1-yl)propyl)-2-(3-(3-fluorophenyl)-1H-indazol-1-yl)acetamide
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N-(3-(dimethylamino)propyl)-2-(3-(3-fluorophenyl)-1H-indazol-1-yl)acetamide
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N-(4-chlorobenzyl)-2-(3-(trifluoromethyl)-4,5,6,7-tetrahydro-1Hindazol-1-yl)acetamide
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N-(4-[methyl[(3-phenyl-1,2,4-oxadiazol-5-yl)methyl]sulfamoyl]phenyl)acetamide
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N-(4-[[(3-phenyl-1,2,4-oxadiazol-5-yl)methyl]sulfamoyl]phenyl)acetamide
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N-(butan-2-yl)-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-(thiophen-2-ylmethyl)-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-cyclohexyl-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-methyl-(3-(dimethylamino)propyl)-2-(3-(3-fluorophenyl)-1H-indazol-1-yl)acetamide
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N-phenyl-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-propyl-2-[3-(trifluoromethyl)-4,5,6,7-tetrahydro-1H-indazol-1-yl]acetamide
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N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]naphthalene-1-sulfonamide
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N-[(5-methyl-2-phenyl-2H-1,2,3-triazol-4-yl)methyl]thiophene-2-sulfonamide
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N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide
N-[4-([[3-(2-chlorophenyl)-1,2,4-oxadiazol-5-yl]methyl]sulfamoyl)phenyl]acetamide
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N-[4-([[3-(2-methylphenyl)-1,2,4-oxadiazol-5-yl]methyl]sulfamoyl)phenyl]acetamide
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tert-butyl-4-(2-(2-(3-(3-fluorophenyl)-1H-indazol-1-yl)acetamido)ethyl)piperazine-1-carboxylate
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tomatine
competitive inhibition versus spermidine, uncompetitive inhibition with respect to ATP and GSH
[3-[4-([6-(3,4-dimethoxyphenyl)-7-[(ethylcarbamothioyl)amino]pyrido[2,3-d]pyrimidin-2-yl]amino)phenyl]propyl]molybdenum(1+)
81.3% activity remaining
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
83.5% activity remaining
1-(1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
90.8% activity remaining
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
85.3% activity remaining
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-hydroxy-3-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
97.4% activity remaining
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
82.1% activity remaining
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
98.7% activity remaining
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(3,4-dimethoxybenzoyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
66.0% activity remaining
1-(6-chloro-1,3-benzothiazol-2-yl)-4-(3,4-dimethoxybenzoyl)-5-(4-fluorophenyl)-3-hydroxy-1,5-dihydro-2H-pyrrol-2-one
99.6% activity remaining
2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide
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2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide
59.0% activity remaining
2-(9-bromo-3-chloro-6-oxo-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl)-N-[2-(methylamino)ethyl]acetamide
55.5% activity remaining
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-1-(6-methoxy-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
77.9% activity remaining
4-(2,3-dihydro-1,4-benzodioxine-6-carbonyl)-3-hydroxy-1-(6-methoxy-1,3-benzothiazol-2-yl)-5-(4-methoxyphenyl)-1,5-dihydro-2H-pyrrol-2-one
97.6% activity remaining
5-oxo-1H,3H-5lambda5-benzo[1,2-c:4,5-c']bis[1,2,5]oxadiazole
7.3% activity remaining
5-oxo-1H,3H-5lambda5-benzo[1,2-c:4,5-c']bis[1,2,5]oxadiazole
63.5% activity remaining
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N,N'-[6-(2,5-dichlorophenyl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
24.3% activity remaining
N,N'-[6-(2,5-dichlorophenyl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
61.3% activity remaining
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N,N'-[6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
25.3% activity remaining
N,N'-[6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidine-2,7-diyl]bis(N'-tert-butylurea)
52.2% activity remaining
N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide
i.e. FS-554, N5-substituted paullone
N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide
i.e. FS-554
N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide
i.e. FS-554
N-[2-(methylamino)ethyl]-2-[6-oxo-9-(trifluoromethyl)-7,12-dihydroindolo[3,2-d][1]benzazepin-5(6H)-yl]acetamide
i.e. FS-554, 40.5% activity remaining
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N-[2-amino-6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-ethylthiourea
20.9% activity remaining
N-[2-amino-6-(2H-1,3-benzodioxol-5-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-ethylthiourea
65.4% activity remaining
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N-[2-amino-6-(naphthalen-2-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-tert-butylurea
48.7% activity remaining
N-[2-amino-6-(naphthalen-2-yl)pyrido[2,3-d]pyrimidin-7-yl]-N'-tert-butylurea
32.3% activity remaining
N1,N10-bis[[4-(propan-2-yl)phenyl]methyl]decane-1,10-diamine
51.1% activity remaining
N1,N10-bis[[4-(propan-2-yl)phenyl]methyl]decane-1,10-diamine
53.5% activity remaining
N1,N12-bis[(4-bromophenyl)methyl]dodecane-1,12-diamine
47.5% activity remaining
N1,N12-bis[(4-bromophenyl)methyl]dodecane-1,12-diamine
30.8% activity remaining
N1,N12-bis[(4-chlorophenyl)methyl]dodecane-1,12-diamine
42.4% activity remaining
N1,N12-bis[(4-chlorophenyl)methyl]dodecane-1,12-diamine
23.8% activity remaining
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N1,N4-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]butane-1,4-diamine
50.9% activity remaining
N1,N4-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]butane-1,4-diamine
25.6% activity remaining
N1,N4-bis[[4-(benzyloxy)phenyl]methyl]butane-1,4-diamine
37.9% activity remaining
N1,N4-bis[[4-(benzyloxy)phenyl]methyl]butane-1,4-diamine
26.6% activity remaining
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N1,N6-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]hexane-1,6-diamine
61.2% activity remaining
N1,N6-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]hexane-1,6-diamine
17.0% activity remaining
N1,N6-bis[[4-(benzyloxy)phenyl]methyl]hexane-1,6-diamine
48.9% activity remaining
N1,N6-bis[[4-(benzyloxy)phenyl]methyl]hexane-1,6-diamine
33.4% activity remaining
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N1,N8-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]octane-1,8-diamine
55.6% activity remaining
N1,N8-bis[[4-(benzyloxy)-3-methoxyphenyl]methyl]octane-1,8-diamine
28.9% activity remaining
limited proteolysis with trypsin or factor Xa result in cleavage of wild-type and mutant enzymes at R553 followed by loss of activity, cleavage of wild-type and mutant R553Q can be delayed by presence of substrates
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additional information
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limited proteolysis with trypsin or factor Xa result in cleavage of wild-type and mutant enzymes at R553 followed by loss of activity, cleavage of wild-type and mutant R553Q can be delayed by presence of substrates
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additional information
screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview. No inhibition by [3-[4-([6-(3,4-dimethoxyphenyl)-7-[(ethylcarbamothioyl)amino]pyrido[2,3-d]pyrimidin-2-yl]amino)phenyl]propyl]molybdenum(1+) and 1,4,7-trioxo-1lambda5,4lambda5,7lambda5-benzo[1,2-c:3,4-c':5,6-c'']tris[1,2,5]oxadiazole
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additional information
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screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview. No inhibition by [3-[4-([6-(3,4-dimethoxyphenyl)-7-[(ethylcarbamothioyl)amino]pyrido[2,3-d]pyrimidin-2-yl]amino)phenyl]propyl]molybdenum(1+) and 1,4,7-trioxo-1lambda5,4lambda5,7lambda5-benzo[1,2-c:3,4-c':5,6-c'']tris[1,2,5]oxadiazole
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additional information
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the enzyme mediates resistance to H2O2 and organic hyperoxids, and to trypanocidic drugs
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additional information
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synthesis and inhibitory potencies of indazole analogue inhibitors, overview
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additional information
screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview. No effect by 8-[(2E)-2-[(2,4-dihydroxyphenyl)methylidene]hydrazinyl]-7-(2-hydroxy-3-phenoxypropyl)-1,3-dimethyl-3,7-dihydro-1H-purine-2,6-dione and J31
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additional information
screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview
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additional information
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screening of different scaffold-derived compounds for inhibitory activity on enzyme TryS, overview
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