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Literature summary extracted from

  • Taha, M.; Aldhamin, E.A.J.; Almandil, N.B.; Anouar, E.H.; Uddin, N.; Alomari, M.; Rahim, F.; Adalat, B.; Ibrahim, M.; Nawaz, F.; Iqbal, N.; Alghanem, B.; Altolayyan, A.; Khan, K.M.
    Synthesis of indole based acetohydrazide analogs Their in vitro and in silico thymidine phosphorylase studies (2020), Bioorg. Chem., 98, 103745 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 2-(2-methyl-1H-indol-3-yl)-N'-(2,4,6-trihydroxybenzylidene)acetohydrazide
-
 Escherichia coli
2.4.2.4 2-(2-methyl-1H-indol-3-yl)-N'-(2-methylbenzylidene)acetohydrazide
-
 Escherichia coli
2.4.2.4 2-(2-methyl-1H-indol-3-yl)-N'-(2-nitrobenzylidene)acetohydrazide
-
 Escherichia coli
2.4.2.4 2-(2-methyl-1H-indol-3-yl)-N'-(3-methylbenzylidene)acetohydrazide
-
 Escherichia coli
2.4.2.4 2-(2-methyl-1H-indol-3-yl)-N'-(3-nitrobenzylidene)acetohydrazide
-
 Escherichia coli
2.4.2.4 2-(2-methyl-1H-indol-3-yl)-N'-(4-methylbenzylidene)acetohydrazide
-
 Escherichia coli
2.4.2.4 2-(2-methyl-1H-indol-3-yl)-N'-(4-nitrobenzylidene)acetohydrazide
-
 Escherichia coli
2.4.2.4 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride TPI Escherichia coli
2.4.2.4 7-deazaxanthine 7DX Escherichia coli
2.4.2.4 methyl-4-((2-(2-(2-methyl-1H-indol-3-yl)acetyl)hydrazono)methyl)benzoate
-
 Escherichia coli
2.4.2.4 additional information synthesis of indole-based acetohydrazide derivatives as inhibitors and molecular docking study using structure with PDB ID 4EAD as template, re-docking of the original ligand 3'-azido-2'-fluoro-dideoxyuridine into the active site. No inhibition by N'-(2,4-dimethoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide Escherichia coli
2.4.2.4 N'-(2,3-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(2,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(2,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(2-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(2-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(3,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(3,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(3-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(3-hydroxy-4-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(3-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(4-(dimethylamino)benzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(4-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli
2.4.2.4 N'-(4-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
 Escherichia coli

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 Escherichia coli
-
 thymidine + phosphate
-
 r

Organism

EC Number Organism UniProt Comment Textmining
2.4.2.4 Escherichia coli P0C037
-
-

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
-
 Escherichia coli thymidine + phosphate
-
 r

Synonyms

EC Number Synonyms Comment Organism
2.4.2.4 ppnP
-
 Escherichia coli
2.4.2.4 pyrimidine/purine nucleoside phosphorylase
-
 Escherichia coli

Temperature Optimum [°C]

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

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
2.4.2.4 7.4
-
 assay at Escherichia coli

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.4 0.0011
-
 pH 7.4, 25°C Escherichia coli 2-(2-methyl-1H-indol-3-yl)-N'-(2,4,6-trihydroxybenzylidene)acetohydrazide
2.4.2.4 0.0012
-
 pH 7.4, 25°C Escherichia coli N'-(2,3-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0014
-
 pH 7.4, 25°C Escherichia coli N'-(3,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0039
-
 pH 7.4, 25°C Escherichia coli N'-(3,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0048
-
 pH 7.4, 25°C Escherichia coli N'-(3-hydroxy-4-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0056
-
 pH 7.4, 25°C Escherichia coli N'-(2,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0066
-
 pH 7.4, 25°C Escherichia coli N'-(2-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0082
-
 pH 7.4, 25°C Escherichia coli N'-(4-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0092
-
 pH 7.4, 25°C Escherichia coli N'-(2,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0116
-
 pH 7.4, 25°C Escherichia coli methyl-4-((2-(2-(2-methyl-1H-indol-3-yl)acetyl)hydrazono)methyl)benzoate
2.4.2.4 0.0132
-
 pH 7.4, 25°C Escherichia coli 2-(2-methyl-1H-indol-3-yl)-N'-(4-nitrobenzylidene)acetohydrazide
2.4.2.4 0.0158
-
 pH 7.4, 25°C Escherichia coli 2-(2-methyl-1H-indol-3-yl)-N'-(2-nitrobenzylidene)acetohydrazide
2.4.2.4 0.0184
-
 pH 7.4, 25°C Escherichia coli N'-(3-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0185
-
 pH 7.4, 25°C Escherichia coli N'-(3-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0199
-
 pH 7.4, 25°C Escherichia coli N'-(4-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0222
-
 pH 7.4, 25°C Escherichia coli 2-(2-methyl-1H-indol-3-yl)-N'-(2-methylbenzylidene)acetohydrazide
2.4.2.4 0.0222
-
 pH 7.4, 25°C Escherichia coli 2-(2-methyl-1H-indol-3-yl)-N'-(3-nitrobenzylidene)acetohydrazide
2.4.2.4 0.0311
-
 pH 7.4, 25°C Escherichia coli N'-(4-(dimethylamino)benzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0361
-
 pH 7.4, 25°C Escherichia coli N'-(2-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
2.4.2.4 0.0381
-
 pH 7.4, 25°C Escherichia coli 2-(2-methyl-1H-indol-3-yl)-N'-(4-methylbenzylidene)acetohydrazide
2.4.2.4 0.03868
-
 pH 7.4, 25°C Escherichia coli 7-deazaxanthine
2.4.2.4 0.0411
-
 pH 7.4, 25°C Escherichia coli 2-(2-methyl-1H-indol-3-yl)-N'-(3-methylbenzylidene)acetohydrazide