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Literature summary extracted from

  • Shahzad, S.A.; Yar, M.; Bajda, M.; Jadoon, B.; Khan, Z.A.; Naqvi, S.A.; Shaikh, A.J.; Hayat, K.; Mahmmod, A.; Mahmood, N.; Filipek, S.
    Synthesis and biological evaluation of novel oxadiazole derivatives: a new class of thymidine phosphorylase inhibitors as potential anti-tumor agents (2014), Bioorg. Med. Chem., 22, 1008-1015.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
2.4.2.4 3-(anilinomethyl)-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(2,3-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(2-chloroanilino)methyl]-5-(2-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(2-chloroanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(2-chloroanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(2-methoxyanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(2-methylanilino)methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(3,4-dichloroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(3,4-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(3-methoxyanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(3-methoxyanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(4-bromoanilino)methyl]-5-(2-bromophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(4-bromoanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[(4-methylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[[(2-phenylethyl)amino]methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 3-[[(4-methoxy-3'-nitro[1,1'-biphenyl]-3-yl)amino]methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 5-(2-bromophenyl)-3-[(2-chloroanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 5-(2-bromophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 5-(4-chlorophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 5-(4-chlorophenyl)-3-[(2-methylanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
-
Escherichia coli
2.4.2.4 5-chloro-6-[1-(2-iminopyrrolidinyl)methyl] uracil hydrochloride
-
Escherichia coli
2.4.2.4 7-deazaxanthine
-
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 thymidine + phosphate Escherichia coli
-
thymine + 2-deoxy-alpha-D-ribose 1-phosphate
-
?

Organism

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

Substrates and Products (Substrate)

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

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
2.4.2.4 0.0144
-
at pH 7.4 and 25°C Escherichia coli 3-[[(4-methoxy-3'-nitro[1,1'-biphenyl]-3-yl)amino]methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.0176
-
at pH 7.4 and 25°C Escherichia coli 5-(2-bromophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.02183
-
at pH 7.4 and 25°C Escherichia coli 5-(2-bromophenyl)-3-[(2-chloroanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.0237
-
at pH 7.4 and 25°C Escherichia coli 3-[(2,3-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.02633
-
at pH 7.4 and 25°C Escherichia coli 3-[(4-bromoanilino)methyl]-5-(2-bromophenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.03868
-
at pH 7.4 and 25°C Escherichia coli 7-deazaxanthine
2.4.2.4 0.04061
-
at pH 7.4 and 25°C Escherichia coli 3-[(3,4-dimethylanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.04064
-
at pH 7.4 and 25°C Escherichia coli 3-[(3-methoxyanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.04638
-
at pH 7.4 and 25°C Escherichia coli 3-[(2-chloroanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.05472
-
at pH 7.4 and 25°C Escherichia coli 3-[(4-methylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.05821
-
at pH 7.4 and 25°C Escherichia coli 5-(4-chlorophenyl)-3-[(2-methylanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.06932
-
at pH 7.4 and 25°C Escherichia coli 3-[[(2-phenylethyl)amino]methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.08319
-
at pH 7.4 and 25°C Escherichia coli 3-[(3,4-dimethylanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.0844
-
at pH 7.4 and 25°C Escherichia coli 3-[(3-methoxyanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.08724
-
at pH 7.4 and 25°C Escherichia coli 3-[(2-methoxyanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.08873
-
at pH 7.4 and 25°C Escherichia coli 5-(4-chlorophenyl)-3-[(2-methoxyanilino)methyl]-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.1041
-
at pH 7.4 and 25°C Escherichia coli 3-(anilinomethyl)-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.1172
-
at pH 7.4 and 25°C Escherichia coli 3-[(2-methylanilino)methyl]-5-(3,4,5-trimethoxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.1177
-
at pH 7.4 and 25°C Escherichia coli 3-[(2-chloroanilino)methyl]-5-phenyl-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.1305
-
at pH 7.4 and 25°C Escherichia coli 3-[(2-chloroanilino)methyl]-5-(2-hydroxyphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.1338
-
at pH 7.4 and 25°C Escherichia coli 3-[(3,4-dichloroanilino)methyl]-5-(4-methylphenyl)-1,3,4-oxadiazole-2(3H)-thione
2.4.2.4 0.1732
-
at pH 7.4 and 25°C Escherichia coli 3-[(4-bromoanilino)methyl]-5-(4-chlorophenyl)-1,3,4-oxadiazole-2(3H)-thione