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Literature summary extracted from

  • Zaman, K.; Rahim, F.; Taha, M.; Wadood, A.; Shah, S.A.A.; Ahmed, Q.U.; Zakaria, Z.A.
    Synthesis of new isoquinoline-base-oxadiazole derivatives as potent inhibitors of thymidine phosphorylase and molecular docking study (2019), Sci. Rep., 9, 16015 .
    View publication on PubMedView publication on EuropePMC

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 (Z)-N'-((4-chloro-2-oxo-4a,8a-dihydro-2H-chromen-3-yl)methylene)-2-oxo-1,2,4a,8a-tetrahydroquinoline-6-carbohydrazide
-
 Homo sapiens
2.4.2.4 3-(3-(quinoxalin-2-yl)thiazolo[2,3-c][1,2,4]triazol-5-yl)benzene-1,2-diol
-
 Homo sapiens
2.4.2.4 4-(2,5-difluorobenzyl)-N-(4-(trifluoromethyl)phenyl)piperazine-1-carbothioamide
-
 Homo sapiens
2.4.2.4 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(1-(4-nitrophenyl)ethylidene)benzohydrazide
-
 Homo sapiens
2.4.2.4 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trihydroxybenzylidene)benzohydrazide
-
 Homo sapiens
2.4.2.4 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trimethoxybenzylidene)benzohydrazide
-
 Homo sapiens
2.4.2.4 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2-nitrobenzylidene)benzohydrazide
-
 Homo sapiens
2.4.2.4 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(3,4,5-trimethoxybenzylidene)benzohydrazide
-
 Homo sapiens
2.4.2.4 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(4-(phenoxymethyl)benzylidene)benzohydrazide
-
 Homo sapiens
2.4.2.4 7-deazaxanthine
-
 Homo sapiens
2.4.2.4 additional information synthesis of isoquinoline-base-oxadiazole derivatives as potent inhibitors of thymidine phosphorylase and molecular docking study, overview. Twenty derivatives of isoquinoline bearing oxadiazole are characterized through different spectroscopic techniques such as HREI-MS, 1H-NMR and 13C-NMR and evaluated for thymidine phosphorylase inhibition, structure-activity relationships study Homo sapiens
2.4.2.4 N'-(2,4-dichlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(2-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(2-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(3,5-dichloro-2-hydroxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(3-aminobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(3-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(3-hydroxy-4-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(4-(dimethylamino)benzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(4-chlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(4-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(4-hydroxy-3,5-dimethoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(4-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(5-bromo-2-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens
2.4.2.4 N'-(anthracen-9-ylmethylene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
-
 Homo sapiens

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
2.4.2.4 thymine + 2-deoxy-alpha-D-ribose 1-phosphate Homo sapiens
-
 thymidine + phosphate
-
 r

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.4 Homo sapiens P19971
-
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
2.4.2.4 thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
 Homo sapiens thymidine + phosphate
-
 r

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
2.4.2.4 25
-
 assay at Homo sapiens

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.2.4 7.4
-
 assay at Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.4 0.0011
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trihydroxybenzylidene)benzohydrazide
2.4.2.4 0.0011
-
 pH 7.4, 25°C Homo sapiens N'-(3-aminobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0024
-
 pH 7.4, 25°C Homo sapiens N'-(3,5-dichloro-2-hydroxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0033
-
 pH 7.4, 25°C Homo sapiens N'-(2,4-dichlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0046
-
 pH 7.4, 25°C Homo sapiens N'-(3-hydroxy-4-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0053
-
 pH 7.4, 25°C Homo sapiens N'-(4-hydroxy-3,5-dimethoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.006
-
 pH 7.4, 25°C Homo sapiens N'-(4-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0063
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2-nitrobenzylidene)benzohydrazide
2.4.2.4 0.0073
-
 pH 7.4, 25°C Homo sapiens N'-(2-hydroxy-3-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0146
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(1-(4-nitrophenyl)ethylidene)benzohydrazide
2.4.2.4 0.0164
-
 pH 7.4, 25°C Homo sapiens N'-(4-chlorobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0185
-
 pH 7.4, 25°C Homo sapiens N'-(2-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0188
-
 pH 7.4, 25°C Homo sapiens N'-(4-(dimethylamino)benzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0221
-
 pH 7.4, 25°C Homo sapiens N'-(4-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0274
-
 pH 7.4, 25°C Homo sapiens N'-(3-cyanobenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0283
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(4-(phenoxymethyl)benzylidene)benzohydrazide
2.4.2.4 0.0367
-
 pH 7.4, 25°C Homo sapiens N'-(5-bromo-2-methoxybenzylidene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.03868
-
 pH 7.4, 25°C Homo sapiens 7-deazaxanthine
2.4.2.4 0.0394
-
 pH 7.4, 25°C Homo sapiens N'-(anthracen-9-ylmethylene)-4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)benzohydrazide
2.4.2.4 0.0473
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(3,4,5-trimethoxybenzylidene)benzohydrazide
2.4.2.4 0.0546
-
 pH 7.4, 25°C Homo sapiens 4-(5-(isoquinolin-3-yl)-1,3,4-oxadiazol-2-yl)-N'-(2,3,4-trimethoxybenzylidene)benzohydrazide

General Information

EC Number General Information Comment Organism
2.4.2.4 malfunction overexpression of thymidine phosphorylase (TP) causes diseases like psoriasis, chronic inflammatory disease, tumor angiogenesis and rheumatoid arthritis etc. The inhibition of this enzyme is vital to secure life from serious threats Homo sapiens