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Literature summary for 3.4.22.51 extracted from

  • Borchhardt, D.; Mascarello, A.; Chiaradia, L.; Nunes, R.; Oliva, G.; Yunes, R.; Andricopulo, A.
    Biochemical evaluation of a series of synthetic chalcone and hydrazide derivatives as novel inhibitors of cruzain from Trypanosoma cruzi (2010), J. Braz. Chem. Soc., 21, 142-150.
No PubMed abstract available
Search for more literature for 3.4.22.51

Application

Application Comment Organism
drug development cruzipain is an attractive target for the development of novel trypanocidal drugs Trypanosoma cruzi

Cloned(Commentary)

Cloned (Comment) Organism
expression of cruzipain truncated in the C-terminal extension in Escherichia coli strains M15 and DH5alpha Trypanosoma cruzi

Inhibitors

Inhibitors Comment Organism Structure
(2E)-1,3-bis(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1,3-di(naphthalen-2-yl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(1,3-benzodioxol-5-yl)-3-(1-naphthyl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2,6-dichlorophenyl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(1,3-benzodioxol-5-yl)-3-(2-chlorophenyl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(1,3-benzodioxol-5-yl)-3-(4-buthoxyphenyl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(1,3-benzodioxol-5-yl)-3-(5-methylfuran-2-yl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(1,3-benzodioxol-5-yl)-3-(thiophen-2-yl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(2',4',5'-trimethoxyphenyl)-3-(thiophen-2-yl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(2'-hydroxy,3'-bromo,4',6'-dimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-buthoxyphenyl)-2-propen-1- one
-
 Trypanosoma cruzi
(2E)-1-(2,4-dimethoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(2-naphthyl)-3-(2,6-dimethoxyphenyl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(2-naphthyl)-3-(5-methylfuran-2-yl)-2-propen-1-one
-
 Trypanosoma cruzi
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3-methoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methylphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-phenylprop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-1-(4-hydroxy-1,3-benzodioxol-5-yl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-(1,3-benzodioxol-5-yl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-(3-methoxyphenyl)-1-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-(4-fluorophenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-3-[4-(benzyloxy)-3-methoxyphenyl]-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
-
 Trypanosoma cruzi
(2E)-N'-(3'-bromo-4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
 Trypanosoma cruzi
(2E)-N'-(4'-buthoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
 Trypanosoma cruzi
(2E)-N'-(4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
-
 Trypanosoma cruzi
3,4,5-trimethoxy-N'-[(E)-(4-nitrophenyl)methylidene]benzohydrazide
-
 Trypanosoma cruzi
3,4,5-trimethoxy-N'-[(E)-naphthalen-1-ylmethylidene]benzohydrazide
-
 Trypanosoma cruzi
E-64
-
 Trypanosoma cruzi
additional information synthesis and inhibitory effects against cruzipaon of a series of thirty-three chalcone and seven hydrazide derivatives, overview Trypanosoma cruzi
N'-[(E)-(2,6-dichlorophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
-
 Trypanosoma cruzi
N'-[(E)-(4-bromophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
-
 Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Bz-Phe-Arg-4-methylcoumaryl-7-amide + H2O
-
 Trypanosoma cruzi Bz-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
cruzain
-
 Trypanosoma cruzi

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
22
-
 assay at room temperature Trypanosoma cruzi

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.5
-
 assay at Trypanosoma cruzi

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.02
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(1,3-benzodioxol-5-yl)-1-(4-bromophenyl)prop-2-en-1-one
0.02
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(4-methoxyphenyl)prop-2-en-1-one
0.02
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(1,3-benzodioxol-5-yl)-3-(2,6-dichlorophenyl)-2-propen-1-one
0.022
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(1,3-benzodioxol-5-yl)-3-(thiophen-2-yl)-2-propen-1-one
0.023
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(1,3-benzodioxol-5-yl)-3-(5-methylfuran-2-yl)-2-propen-1-one
0.025
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(4-hydroxy-1,3-benzodioxol-5-yl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
0.025
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(1,3-benzodioxol-5-yl)-3-(1-naphthyl)-2-propen-1-one
0.025
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(1,3-benzodioxol-5-yl)-3-(2-chlorophenyl)-2-propen-1-one
0.025
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(2-naphthyl)-3-(2,6-dimethoxyphenyl)-2-propen-1-one
0.025
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1,3-di(naphthalen-2-yl)prop-2-en-1-one
0.025
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(2-naphthyl)-3-(5-methylfuran-2-yl)-2-propen-1-one
0.03
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(4-bromophenyl)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)prop-2-en-1-one
0.03
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methylphenyl)prop-2-en-1-one
0.035
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(4-methoxyphenyl)prop-2-en-1-one
0.037
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(2'-hydroxy,3'-bromo,4',6'-dimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
0.037
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-[4-(benzyloxy)-3-methoxyphenyl]-1-(2,4-dimethoxyphenyl)prop-2-en-1-one
0.04
-
 pH 6.5, 22°C Trypanosoma cruzi 3,4,5-trimethoxy-N'-[(E)-naphthalen-1-ylmethylidene]benzohydrazide
0.045
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(3-bromo-2-hydroxy-4,6-dimethoxyphenyl)-3-(3-nitrophenyl)prop-2-en-1-one
0.046
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(1,3-benzodioxol-5-yl)-3-(4-buthoxyphenyl)-2-propen-1-one
0.047
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-N'-(4'-buthoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
0.048
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(2',4',5'-trimethoxyphenyl)-3-(1-naphthyl)-2-propen-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-phenylprop-2-en-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(3a,7a-dihydro-1,3-benzodioxol-5-yl)-3-(3-methoxyphenyl)prop-2-en-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(1,3-benzodioxol-5-yl)-3-(3-methoxy-4-phenoxyphenyl)prop-2-en-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(4-fluorophenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(1,3-benzodioxol-5-yl)-1-(naphthalen-2-yl)prop-2-en-1-one
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-N'-(3'-bromo-4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-N'-(4'-hydroxy-5'-methoxybenzilidene)-3,4,5-trimethoxybenzohydrazide
0.05
-
 pH 6.5, 22°C Trypanosoma cruzi N'-[(E)-(2,6-dichlorophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
0.055
-
 pH 6.5, 22°C Trypanosoma cruzi N'-[(E)-(4-bromophenyl)methylidene]-3,4,5-trimethoxybenzohydrazide
0.06
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(4-methoxyphenyl)-1-(naphthalen-2-yl)prop-2-en-1-one
0.06
-
 pH 6.5, 22°C Trypanosoma cruzi 3,4,5-trimethoxy-N'-[(E)-(4-nitrophenyl)methylidene]benzohydrazide
0.082
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(2'-hydroxy-3'-bromo-4',6'-dimethoxyphenyl)-3-(4-buthoxyphenyl)-2-propen-1- one
0.1
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(1,3-benzodioxol-5-yl)-1-(2-hydroxyphenyl)prop-2-en-1-one
0.1
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1,3-bis(2,4,5-trimethoxyphenyl)prop-2-en-1-one
0.1
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(2',4',5'-trimethoxyphenyl)-3-(thiophen-2-yl)-2-propen-1-one
0.1
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-3-(3-methoxyphenyl)-1-(2,4,5-trimethoxyphenyl)prop-2-en-1-one
0.1
-
 pH 6.5, 22°C Trypanosoma cruzi (2E)-1-(2,4-dimethoxyphenyl)-3-(2,4,5-trimethoxyphenyl)prop-2-en-1-one