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Literature summary extracted from

  • Alvarez, G.; Aguirre-Lopez, B.; Varela, J.; Cabrera, M.; Merlino, A.; Lopez, G.V.; Lavaggi, M.L.; Porcal, W.; Di Maio, R.; Gonzalez, M.; Cerecetto, H.; Cabrera, N.; Perez-Montfort, R.; de Gomez-Puyou, M.T.; Gomez-Puyou, A.
    Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity (2010), Eur. J. Med. Chem., 45, 5767-5772.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
5.3.1.1 (1Z,2Z)-N,N'-dihydroxy-4-methylcyclohexa-3,5-diene-1,2-diimine
-
 Trypanosoma cruzi
5.3.1.1 (2E)-2-[(4-methyl-5-oxido-1,2,5-oxadiazol-3-yl)methylidene]hydrazinecarbothioamide
-
 Trypanosoma cruzi
5.3.1.1 (2E)-2-[(5-nitrofuran-2-yl)methylidene]hydrazinecarbothioamide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 (2E)-2-[2-[(3-oxido-2,1,3-benzoxadiazol-5-yl)methoxy]benzylidene]-N-(prop-2-en-1-yl)hydrazinecarbothioamide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 (2E)-N-(naphthalen-2-yl)-2-[(2E)-3-(5-nitrofuran-2-yl)prop-2-en-1-ylidene]hydrazinecarboxamide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 (2E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[(5-nitrofuran-2-yl)methylidene]hydrazinecarboxamide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 (4-methyl-1,2,3-thiadiazol-5-yl)methanol 29% inhibition at 0.4 mM Trypanosoma cruzi
5.3.1.1 1,2,4-thiadiazole 59% inhibition at 0.1 mM Homo sapiens
5.3.1.1 1,2,4-thiadiazole
-
 Trypanosoma cruzi
5.3.1.1 1,2,6-thiadiazine irreversible inhibitor Trypanosoma cruzi
5.3.1.1 1,3,4-oxathiazole
-
 Trypanosoma cruzi
5.3.1.1 2,6-dibenzyl-4-[(5-nitrothiophen-2-yl)methylidene]-1,2,6-thiadiazinane-3,5-dione 1,1-dioxide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 2-phenyl-4H-chromen-4-one
-
 Trypanosoma cruzi
5.3.1.1 2-[(1E)-2-nitroprop-1-en-1-yl]thiophene
-
 Trypanosoma cruzi
5.3.1.1 2-[(3-aminophenyl)disulfanyl]aniline
-
 Trypanosoma cruzi
5.3.1.1 3,5-diphenyl-1,2,4-thiadiazole 74% inhibition at 0.4 mM Trypanosoma cruzi
5.3.1.1 3-(4-methylphenyl)-5-[(4-methylphenyl)sulfonyl]-1,2,4-thiadiazole
-
 Trypanosoma cruzi
5.3.1.1 3-nitrobiphenyl-4-amine
-
 Trypanosoma cruzi
5.3.1.1 4-(4-nitrobenzylidene)-2,6-bis(2-phenylethyl)-1,2,6-thiadiazinane-3,5-dione 1,1-dioxide irreversible inhibitor, 85% inhibition at 0.4 mM Trypanosoma cruzi
5.3.1.1 4-[(5-nitrofuran-2-yl)methylidene]-4H-1,2,6-thiadiazine-3,5-diamine 1,1-dioxide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 4-[(5-nitrothiophen-2-yl)methylidene]-2,6-bis(2-phenylethyl)-1,2,6-thiadiazinane-3,5-dione 1,1-dioxide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 5-[(1E)-2-nitroprop-1-en-1-yl]-1,3-benzodioxole
-
 Trypanosoma cruzi
5.3.1.1 6,6'-bi-1,3-benzothiazole-2,2'-diamine
-
 Trypanosoma cruzi
5.3.1.1 6-[(E)-2-(5-nitrothiophen-2-yl)ethenyl]-2,1,3-benzoxadiazole 1-oxide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 6-[(E)-2-[(4-fluorophenyl)sulfanyl]ethenyl]-2,1,3-benzoxadiazole 1-oxide irreversible inhibitor Trypanosoma cruzi
5.3.1.1 8-bromo-5,10-dioxidophenazin-2-yl chloroacetate 50% inhibition at 0.4 mM Trypanosoma cruzi
5.3.1.1 ethyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,2,4-thiadiazole-5-carboxylate
-
 Trypanosoma cruzi
5.3.1.1 ethyl 3-phenyl-1,2,4-thiadiazole-5-carboxylate
-
 Trypanosoma cruzi
5.3.1.1 additional information not inhibited by 1,2,6-thiadiazine, phenazine 5,9-dioxide, and 1,3,4-oxathiazole Homo sapiens
5.3.1.1 N-[(2-oxido-4-phenyl-1,2,5-oxadiazol-3-yl)methyl]naphthalen-1-amine 72% inhibition at 0.4 mM Trypanosoma cruzi
5.3.1.1 N-[(4-methyl-5-oxido-1,2,5-oxadiazol-3-yl)methyl]naphthalen-1-amine 41% inhibition at 0.4 mM Trypanosoma cruzi
5.3.1.1 phenazine 5,9-dioxide 84% inhibition at 0.4 mM Trypanosoma cruzi

Organism

EC Number Organism UniProt Comment Textmining
5.3.1.1 Homo sapiens
-
-
-
5.3.1.1 Trypanosoma cruzi
-
-
-
5.3.1.1 Trypanosoma cruzi T2
-
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
5.3.1.1 D-glyceraldehyde 3-phosphate
-
 Homo sapiens dihydroxyacetone phosphate
-
 ?
5.3.1.1 D-glyceraldehyde 3-phosphate
-
 Trypanosoma cruzi dihydroxyacetone phosphate
-
 ?
5.3.1.1 D-glyceraldehyde 3-phosphate
-
 Trypanosoma cruzi T2 dihydroxyacetone phosphate
-
 ?

Synonyms

EC Number Synonyms Comment Organism
5.3.1.1 TIM
-
 Homo sapiens
5.3.1.1 TIM
-
 Trypanosoma cruzi
5.3.1.1 Triosephosphate isomerase
-
 Homo sapiens
5.3.1.1 Triosephosphate isomerase
-
 Trypanosoma cruzi

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
5.3.1.1 0.0035
-
 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 1,2,4-thiadiazole
5.3.1.1 0.01
-
 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 1,3,4-oxathiazole
5.3.1.1 0.013
-
 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 1,2,6-thiadiazine
5.3.1.1 0.02
-
 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 4-[(5-nitrofuran-2-yl)methylidene]-4H-1,2,6-thiadiazine-3,5-diamine 1,1-dioxide
5.3.1.1 0.026
-
 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi phenazine 5,9-dioxide
5.3.1.1 0.03 0.1 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 6-[(E)-2-(5-nitrothiophen-2-yl)ethenyl]-2,1,3-benzoxadiazole 1-oxide
5.3.1.1 0.03 0.1 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi (2E)-N-[2-(3,4-dimethoxyphenyl)ethyl]-2-[(5-nitrofuran-2-yl)methylidene]hydrazinecarboxamide
5.3.1.1 0.03 0.1 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 2,6-dibenzyl-4-[(5-nitrothiophen-2-yl)methylidene]-1,2,6-thiadiazinane-3,5-dione 1,1-dioxide
5.3.1.1 0.03 0.1 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi ethyl 3-phenyl-1,2,4-thiadiazole-5-carboxylate
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 6-[(E)-2-[(4-fluorophenyl)sulfanyl]ethenyl]-2,1,3-benzoxadiazole 1-oxide
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi (2E)-2-[2-[(3-oxido-2,1,3-benzoxadiazol-5-yl)methoxy]benzylidene]-N-(prop-2-en-1-yl)hydrazinecarbothioamide
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 4-(4-nitrobenzylidene)-2,6-bis(2-phenylethyl)-1,2,6-thiadiazinane-3,5-dione 1,1-dioxide
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi ethyl 3-(3,5-di-tert-butyl-4-hydroxyphenyl)-1,2,4-thiadiazole-5-carboxylate
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 3-(4-methylphenyl)-5-[(4-methylphenyl)sulfonyl]-1,2,4-thiadiazole
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi (2E)-N-(naphthalen-2-yl)-2-[(2E)-3-(5-nitrofuran-2-yl)prop-2-en-1-ylidene]hydrazinecarboxamide
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi (2E)-2-[(5-nitrofuran-2-yl)methylidene]hydrazinecarbothioamide
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 4-[(5-nitrothiophen-2-yl)methylidene]-2,6-bis(2-phenylethyl)-1,2,6-thiadiazinane-3,5-dione 1,1-dioxide
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 3,5-diphenyl-1,2,4-thiadiazole
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 2-phenyl-4H-chromen-4-one
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi (2E)-2-[(4-methyl-5-oxido-1,2,5-oxadiazol-3-yl)methylidene]hydrazinecarbothioamide
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi N-[(2-oxido-4-phenyl-1,2,5-oxadiazol-3-yl)methyl]naphthalen-1-amine
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 2-[(1E)-2-nitroprop-1-en-1-yl]thiophene
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 5-[(1E)-2-nitroprop-1-en-1-yl]-1,3-benzodioxole
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi (1Z,2Z)-N,N'-dihydroxy-4-methylcyclohexa-3,5-diene-1,2-diimine
5.3.1.1 0.1
-
 IC50 about 0.1 mM, in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 3-nitrobiphenyl-4-amine
5.3.1.1 0.4
-
 in 100 mM triethanolamine, 10 mM EDTA, pH 7.4 and 10% of dimethyl sulfoxide, at 36°C Trypanosoma cruzi 8-bromo-5,10-dioxidophenazin-2-yl chloroacetate