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Literature summary for 3.4.22.51 extracted from

  • Pizzo, C.; Saiz, C.; Talevi, A.; Gavernet, L.; Palestro, P.; Bellera, C.; Blanch, L.B.; Benitez, D.; Cazzulo, J.J.; Chidichimo, A.; Wipf, P.; Mahler, S.G.
    Synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma cruzi (2011), Chem. Biol. Drug Des., 77, 166-172.
    View publication on PubMed
Search for more literature for 3.4.22.51

Inhibitors

Inhibitors Comment Organism Structure
2-[(2Z)-2-[(2Z)-(3-bromobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide 17% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
2-[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide 7% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
2-[(2Z)-2-[(2Z)-(4-fluorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide 3% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
2-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide 22% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
2-[(2Z)-2-[(2Z)-benzylidenehydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide 3% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
2-[(2Z)-2-[(2Z)-[1-(3-bromophenyl)ethylidene]hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-yl]-N-methylacetamide 22% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
E-64 complete inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
methyl (2E)-[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate 75% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
methyl (2E)-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-3-methyl-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate 71% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
methyl (2E)-[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-ylidene]ethanoate 7% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
methyl (2E)-[(2Z)-3-methyl-4-oxo-2-[(2Z)-[4-(trifluoromethyl)benzylidene]hydrazinylidene]-1,3-thiazolidin-5-ylidene]ethanoate 65% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
additional information synthesis of 2-hydrazolyl-4-thiazolidinones based on multicomponent reactions and biological evaluation against Trypanosoma cruzi, inhibitory potencies and cytotoxic effects, molecular modeling and QSAR studies, overview. No inhibition by (RS)-2-(2-(2-bromobenzylidene)hydrazono)-3-methyl-4-oxo-5-thiazolidine-N-methylacetamide and (Z)-((2-(4-fluorobenzylidene)hydrazono)-3-methyl-5-methoxycarbonylmethylene)thiazolidin-4-one at 0.1 mM Trypanosoma cruzi
N-methyl-2-[(2Z)-3-methyl-4-oxo-2-[(2Z)-[4-(trifluoromethyl)benzylidene]hydrazinylidene]-1,3-thiazolidin-5-yl]acetamide 27% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
N-methyl-2-[(2Z)-4-oxo-2-[(2Z)-(2-sulfanylbenzylidene)hydrazinylidene]-1,3-thiazolidin-5-yl]acetamide 27% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
[(2Z)-2-[(2Z)-(2-fluorobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid 6% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
[(2Z)-2-[(2Z)-(4-chlorobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid 11% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
[(2Z)-2-[(2Z)-(4-methoxybenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid 38% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
[(2Z)-2-[(2Z)-(4-nitrobenzylidene)hydrazinylidene]-4-oxo-1,3-thiazolidin-5-yl]acetic acid 4% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi
[(2Z)-4-oxo-2-[(2Z)-(thiophen-2-ylmethylidene)hydrazinylidene]-1,3-thiazolidin-5-yl]acetic acid 34% inhibition at 0.1 mM inhibitor and 140 nM enzyme Trypanosoma cruzi

Organism

Organism UniProt Comment Textmining
Trypanosoma cruzi
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Bz-Pro-Phe-Arg-4-nitroanilide + H2O
-
 Trypanosoma cruzi Bz-Pro-Phe-Arg + 4-nitroaniline
-
 ?

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
 assay at Trypanosoma cruzi

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.6
-
 assay at Trypanosoma cruzi