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Literature summary for 2.4.2.4 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

Inhibitors Comment Organism Structure
2-(2-methyl-1H-indol-3-yl)-N'-(2,4,6-trihydroxybenzylidene)acetohydrazide
-
Escherichia coli
2-(2-methyl-1H-indol-3-yl)-N'-(2-methylbenzylidene)acetohydrazide
-
Escherichia coli
2-(2-methyl-1H-indol-3-yl)-N'-(2-nitrobenzylidene)acetohydrazide
-
Escherichia coli
2-(2-methyl-1H-indol-3-yl)-N'-(3-methylbenzylidene)acetohydrazide
-
Escherichia coli
2-(2-methyl-1H-indol-3-yl)-N'-(3-nitrobenzylidene)acetohydrazide
-
Escherichia coli
2-(2-methyl-1H-indol-3-yl)-N'-(4-methylbenzylidene)acetohydrazide
-
Escherichia coli
2-(2-methyl-1H-indol-3-yl)-N'-(4-nitrobenzylidene)acetohydrazide
-
Escherichia coli
5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride TPI Escherichia coli
7-deazaxanthine 7DX Escherichia coli
methyl-4-((2-(2-(2-methyl-1H-indol-3-yl)acetyl)hydrazono)methyl)benzoate
-
Escherichia coli
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
N'-(2,3-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(2,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(2,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(2-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(2-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(3,4-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(3,5-dihydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(3-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(3-hydroxy-4-methoxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(3-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(4-(dimethylamino)benzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(4-chlorobenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli
N'-(4-hydroxybenzylidene)-2-(2-methyl-1H-indol-3-yl)acetohydrazide
-
Escherichia coli

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
thymine + 2-deoxy-alpha-D-ribose 1-phosphate Escherichia coli
-
thymidine + phosphate
-
r

Organism

Organism UniProt Comment Textmining
Escherichia coli P0C037
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
Escherichia coli thymidine + phosphate
-
r

Synonyms

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

Temperature Optimum [°C]

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

pH Optimum

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

IC50 Value

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