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Literature summary for 3.4.22.51 extracted from

  • Herrera-Mayorga, V.; Lara-Ramirez, E.E.; Chacon-Vargas, K.F.; Aguirre-Alvarado, C.; Rodriguez-Paez, L.; Alcantara-Farfan, V.; Cordero-Martinez, J.; Nogueda-Torres, B.; Reyes-Espinosa, F.; Bocanegra-Garcia, V.; Rivera, G.
    Structure-based virtual screening and in vitro evaluation of new Trypanosoma cruzi cruzain inhibitors (2019), Int. J. Mol. Sci., 20, E1742 .
    View publication on PubMedView publication on EuropePMC
Search for more literature for 3.4.22.51

Inhibitors

Inhibitors Comment Organism Structure
(5R)-5-(3,4-difluorophenyl)-3-[2-[(5S)-5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]-5-methylimidazolidine-2,4-dione in the epimastigote form, the inhibitor does not show trypanocidal effects, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM Trypanosoma cruzi
1-[(5R)-3,5-di(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-2-([5-[(5S)-5-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)ethanone in the epimastigote form, the inhibitor does not show trypanocidal effects, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM Trypanosoma cruzi
4-amino-6-methyl-3-([2-[(5R)-3-(naphthalen-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]sulfanyl)-1,2,4-triazin-5(4H)-one shows trypanocidal activity, promising structure in the search for new agents to treat Chagas disease Trypanosoma cruzi
N-[4-methyl-3-(piperidin-1-ylsulfonyl)phenyl]-4-oxo-4-(3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)butanamide weak inhibitor shows trypanocidal activity, against bloodstream trypomastigotes the LC50 value is greater than 0.250 mM Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi P25779
-
-
Trypanosoma cruzi INC-5 P25779
-
-

Source Tissue

Source Tissue Comment Organism Textmining
epimastigote
-
 Trypanosoma cruzi
-
trypomastigote
-
 Trypanosoma cruzi
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Trypanosoma cruzi benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?
benzyloxycarbonyl-Phe-Arg-7-amido-4-methylcoumarin + H2O
-
 Trypanosoma cruzi INC-5 benzyloxycarbonyl-Phe-Arg + 7-amino-4-methylcoumarin
-
 ?

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
0.05035
-
 23°C, pH 6.8 Trypanosoma cruzi (5R)-5-(3,4-difluorophenyl)-3-[2-[(5S)-5-(furan-2-yl)-3-(4-methylphenyl)-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]-5-methylimidazolidine-2,4-dione
0.05623
-
 23°C, pH 6.7 Trypanosoma cruzi 4-amino-6-methyl-3-([2-[(5R)-3-(naphthalen-2-yl)-5-phenyl-4,5-dihydro-1H-pyrazol-1-yl]-2-oxoethyl]sulfanyl)-1,2,4-triazin-5(4H)-one
0.08437
-
 23°C, pH 6.6 Trypanosoma cruzi 1-[(5R)-3,5-di(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl]-2-([5-[(5S)-5-methyl-4,5,6,7-tetrahydro-1-benzothiophen-2-yl]-1,3,4-oxadiazol-2-yl]sulfanyl)ethanone
1.41
-
 23°C, pH 6.5 Trypanosoma cruzi N-[4-methyl-3-(piperidin-1-ylsulfonyl)phenyl]-4-oxo-4-(3-phenyl-4,5-dihydro-1H-pyrazol-1-yl)butanamide