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Literature summary for 3.4.22.16 extracted from

  • Garg, S.; Raghav, N.
    2,5-Diaryloxadiazoles and their precursors as novel inhibitors of cathepsins B, H and L (2016), Bioorg. Chem., 67, 64-74 .
    View publication on PubMed
Search for more literature for 3.4.22.16

Inhibitors

Inhibitors Comment Organism Structure
1-[4-(2-methoxyphenyl)piperazin-1-yl]-3-[3-(5-methyl-1,3,4-oxadiazol-2-yl)phenoxy]propan-2-ol
-
 Capra hircus
2,5-diphenyl-1,3,4-oxadiazole 1 mM, 50.19% activity remaining Capra hircus
2-(2-chlorophenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 25.12% activity remaining Capra hircus
2-(2-methoxyphenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 45.35% activity remaining Capra hircus
2-(2-nitrophenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 92.07% activity remaining Capra hircus
2-(3-chlorophenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 36.19% activity remaining Capra hircus
2-(3-methoxyphenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 48.08% activity remaining Capra hircus
2-(3-nitrophenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 59.47% activity remaining Capra hircus
2-(4-chlorophenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 30.98% activity remaining Capra hircus
2-(4-methoxyphenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 43.49% activity remaining Capra hircus
2-(4-methylphenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 49.89% activity remaining Capra hircus
2-(4-nitrophenyl)-5-phenyl-1,3,4-oxadiazole 1 mM, 69.33% activity remaining Capra hircus
2-benzyl-N'-methyl-N'-(pyridin-3-yl)but-3-ynehydrazide
-
 Capra hircus
2-[[(2E)-2-(1,3-benzodioxol-5-ylmethylidene)hydrazinyl]carbonyl]-3-phenyl-1H-indole-5-sulfonamide
-
 Capra hircus
4-bromo-N-[(2-methylimidazo[1,2-a]pyridin-3-yl)carbonyl]benzenecarbohydrazonoyl chloride
-
 Capra hircus
Leu-CH2Cl
-
 Capra hircus
additional information 2,5-diaryloxadiazoles and their precursors as inhibitors of cathepsins B, H and L, synthesis and inhibitory potencies, pharmacological evaluation, molecular docking, overview. Structure-activity relationship studies show that 2,5-diaryloxadiazoles are less inhibitory than their precursors, N-subsituted benzylidenebenzohydrazides. Cathepsin H activity is maximally inhibited by (2E)-3-(3-methoxyphenyl)-1-phenylprop-2-en-1-one and (2Z)-2-[(2E)-3-(4-chlorophenyl)-1-phenylprop-2-en-1-ylidene]hydrazinecarboxamide, assay with liver hommogenate. All compounds exhibited a competitive type of inhibition Capra hircus
N'-(4-[(E)-[2-(2-formylphenyl)hydrazinylidene]methyl]phenyl)-N-phenylimidoformamide
-
 Capra hircus
N-(3-methoxypyrazin-2-yl)-2-[4-(1,3,4-oxadiazol-2-yl)phenyl]pyridine-3-sulfonamide
-
 Capra hircus
N-benzyl-5-hydroxy-1-methyl-2-[2-[(1,3,4-oxadiazol-2-ylcarbonyl)amino]propan-2-yl]-6-oxo-1,6-dihydropyrimidine-4-carboxamide
-
 Capra hircus
N-[(1E,2S)-1-(2-benzoylhydrazinylidene)-4-phenylbutan-2-yl]-N2-(piperidin-1-ylcarbonyl)-L-leucinamide
-
 Capra hircus
N-[(5S,8S,11S,13Z,19S)-8-(4-fluorobenzyl)-5-formyl-2,7,10-trioxo-18-oxa-1,6,9-triazabicyclo[17.2.1]docos-13-en-11-yl]-5-methyl-1,2-oxazole-3-carboxamide
-
 Capra hircus
N-[(E)-(phenylimino)methyl]benzamide 1 mM, 69.90% activity remaining Capra hircus
N-[(E)-[(2-chlorophenyl)imino]methyl]benzamide 1 mM, 25.66% activity remaining Capra hircus
N-[(E)-[(2-methoxyphenyl)imino]methyl]benzamide 1 mM, 41.11% activity remaining Capra hircus
N-[(E)-[(2-nitrophenyl)imino]methyl]benzamide 1 mM, 90.07% activity remaining Capra hircus
N-[(E)-[(3-chlorophenyl)imino]methyl]benzamide 1 mM, 39.45% activity remaining Capra hircus
N-[(E)-[(3-methoxyphenyl)imino]methyl]benzamide 1 mM, 49.59% activity remaining Capra hircus
N-[(E)-[(3-nitrophenyl)imino]methyl]benzamide 1 mM, 73.01% activity remaining Capra hircus
N-[(E)-[(4-chlorophenyl)imino]methyl]benzamide 1 mM, 24.75% activity remaining Capra hircus
N-[(E)-[(4-methoxyphenyl)imino]methyl]benzamide 1 mM, 40.2% activity remaining Capra hircus
N-[(E)-[(4-methylphenyl)imino]methyl]benzamide 1 mM, 39.93% activity remaining Capra hircus
N-[(E)-[(4-nitrophenyl)imino]methyl]benzamide 1 mM, 75.07% activity remaining Capra hircus
N-[2-(4-methoxyphenyl)ethyl]-2-(2-phenoxyphenyl)acetamide
-
 Capra hircus

Localization

Localization Comment Organism GeneOntology No. Textmining
lysosome
-
 Capra hircus 5764
-

Organism

Organism UniProt Comment Textmining
Capra hircus A0A060INS8
-
-

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
 Capra hircus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
Leu-2-naphthylamide + H2O
-
 Capra hircus leucine + 2-naphthylamine
-
 ?

Synonyms

Synonyms Comment Organism
CTSH
-
 Capra hircus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Capra hircus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5
-
 assay at Capra hircus

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.00044
-
 N-[(E)-[(4-chlorophenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00056
-
 2-(2-chlorophenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00068
-
 N-[(E)-[(2-chlorophenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.001
-
 2-(4-chlorophenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00113
-
 2-(3-chlorophenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00113
-
 N-[(E)-[(3-chlorophenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00126
-
 N-[(E)-[(4-methylphenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00133
-
 2-(4-methoxyphenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00133
-
 N-[(E)-[(4-methoxyphenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.0014
-
 N-[(E)-[(2-methoxyphenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00147
-
 2-(2-methoxyphenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00161
-
 2-(3-methoxyphenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00168
-
 N-[(E)-[(3-methoxyphenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00214
-
 N-[(E)-(phenylimino)methyl]benzamide pH 5.0, 37°C Capra hircus
0.00255
-
 2-(4-methylphenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00272
-
 2,5-diphenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00364
-
 N-[(E)-[(3-nitrophenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00385
-
 2-(3-nitrophenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00416
-
 N-[(E)-[(4-nitrophenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00484
-
 N-[(E)-[(2-nitrophenyl)imino]methyl]benzamide pH 5.0, 37°C Capra hircus
0.00496
-
 2-(4-nitrophenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus
0.00669
-
 2-(2-nitrophenyl)-5-phenyl-1,3,4-oxadiazole pH 5.0, 37°C Capra hircus