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Literature summary extracted from

  • Zanatta, N.; Amaral, S.S.; Dos Santos, J.M.; de Mello, D.L.; Fernandes, L.d.a..S.; Bonacorso, H.G.; Martins, M.A.; Andricopulo, A.D.; Borchhardt, D.M.
    Convergent synthesis and cruzain inhibitory activity of novel 2-(N-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines (2008), Bioorg. Med. Chem., 16, 10236-10243.
    View publication on PubMed

Cloned(Commentary)

EC Number Cloned (Comment) Organism
3.4.22.51 expression in Escherichia coli strain DH5alpha Trypanosoma cruzi

Inhibitors

EC Number Inhibitors Comment Organism Structure
3.4.22.51 2-(N-1-phenyl-ethylidenehydrazino)-4-trifluoromethylpyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-1-phenyl-ethylidenehydrazino)-5-methyl-4-trifluoro-methyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-1-phenyl-ethylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-2-hydroxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-2-hydroxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-2-hydroxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-2-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-2-methoxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-2-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine 100 microM, 20% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-2-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine 100 microM, 45% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-2-methyl-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-2-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine 100 microM, 45% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-4-chloro-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine 100 microM, 80% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-4-chloro-benzylidenehydrazino)-5-methyl-4-trifluoro-methyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-4-chloro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine 100 microM, 60% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-4-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine 100 microM, 40% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-4-methoxy-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-4-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-4-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine 100 microM, 40% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-4-methyl-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-4-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-4-nitro-benzylidenehydrazino)-4-trifluoromethylpyrimidine 100 microM, 50% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-4-nitro-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-4-nitro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-benzylidenehydrazino)-4-trifluoromethylpyrimidine 100 microM, 30% inhibitory effect Trypanosoma cruzi
3.4.22.51 2-(N-benzylidenehydrazino)-5-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 2-(N-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine 100 microM Trypanosoma cruzi
3.4.22.51 trans-epoxysuccinyl-L-leucylamido-(4-guanidino)butane irreversible inhibitor Trypanosoma cruzi

Organism

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

Synonyms

EC Number Synonyms Comment Organism
3.4.22.51 cruzain
-
 Trypanosoma cruzi

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
3.4.22.51 additional information
-
 assay at room temperature, pH 6.5, 5 min, 0.64 nM cruzain, 50 mM sodium phosphate, 100 mM sodium chloride, 5 mM EDTA Trypanosoma cruzi

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
3.4.22.51 6.5
-
 assay at room temperature, 5 min, 0.64 nM cruzain, 50 mM sodium phosphate, 100 mM sodium chloride, 5 mM EDTA Trypanosoma cruzi

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
3.4.22.51 0.085
-
-
 Trypanosoma cruzi 2-(N-4-chloro-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
3.4.22.51 0.1
-
 about 0.1 mM Trypanosoma cruzi 2-(N-4-nitro-benzylidenehydrazino)-4-trifluoromethylpyrimidine
3.4.22.51 0.1
-
 about 0.1 mM Trypanosoma cruzi 2-(N-4-chloro-benzylidenehydrazino)-6-methyl-4-trifluoro-methyl-pyrimidine
3.4.22.51 0.1
-
 above 0.1 mM Trypanosoma cruzi 2-(N-2-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
3.4.22.51 0.1
-
 above 0.1 mM Trypanosoma cruzi 2-(N-4-methyl-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
3.4.22.51 0.1
-
 above 0.1 mM Trypanosoma cruzi 2-(N-4-methoxy-benzylidenehydrazino)-4-trifluoromethyl-pyrimidine
3.4.22.51 0.1
-
 above 0.1 mM Trypanosoma cruzi 2-(N-2-methyl-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine
3.4.22.51 0.15
-
 above 0.15 mM Trypanosoma cruzi 2-(N-benzylidenehydrazino)-4-trifluoromethylpyrimidine
3.4.22.51 0.15
-
 above 0.15 mM Trypanosoma cruzi 2-(N-2-methoxy-benzylidenehydrazino)-6-methyl-4-trifluoromethyl-pyrimidine