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Literature summary extracted from

  • Sathisha, K.R.; Khanum, S.A.; Chandra, J.N.; Ayisha, F.; Balaji, S.; Marathe, G.K.; Gopal, S.; Rangappa, K.S.
    Synthesis and xanthine oxidase inhibitory activity of 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives (2011), Bioorg. Med. Chem., 19, 211-220.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.17.3.2 2-[(2,3-dimethylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(2,3-dimethylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(2,4-dimethylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(2,4-dimethylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(2-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(2-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(2-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(2-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(2-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(2-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(3-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(3-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(3-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(3-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(3-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(3-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(4-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(4-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(4-chloro-3-methylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(4-chloro-3-methylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(4-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(4-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(4-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(4-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 2-[(4-methoxyphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 2-[(4-methoxyphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 7-methyl-2-[(2-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 7-methyl-2-[(2-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 7-methyl-2-[(2-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 7-methyl-2-[(2-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 7-methyl-2-[(3-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 7-methyl-2-[(3-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 7-methyl-2-[(3-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 7-methyl-2-[(3-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 7-methyl-2-[(4-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 7-methyl-2-[(4-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 7-methyl-2-[(4-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Bos taurus
1.17.3.2 7-methyl-2-[(4-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
-
 Rattus norvegicus
1.17.3.2 allopurinol
-
 Bos taurus
1.17.3.2 allopurinol
-
 Rattus norvegicus
1.17.3.2 additional information synthesis and inhibitory activity of 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives, molecular modeling and docking studies, overview Bos taurus
1.17.3.2 additional information synthesis and inhibitory activity of 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one derivatives, molecular modeling and docking studies, overview Rattus norvegicus

Localization

EC Number Localization Comment Organism GeneOntology No. Textmining
1.17.3.2 extracellular
-
 Bos taurus
-
-

Natural Substrates/ Products (Substrates)

EC Number Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
1.17.3.2 xanthine + H2O + O2 Rattus norvegicus
-
 urate + H2O2
-
 ?
1.17.3.2 xanthine + H2O + O2 Bos taurus
-
 urate + H2O2
-
 ?

Organism

EC Number Organism UniProt Comment Textmining
1.17.3.2 Bos taurus
-
-
-
1.17.3.2 Rattus norvegicus
-
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.17.3.2 liver
-
 Rattus norvegicus
-
1.17.3.2 milk
-
 Bos taurus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.17.3.2 xanthine + H2O + O2
-
 Rattus norvegicus urate + H2O2
-
 ?
1.17.3.2 xanthine + H2O + O2
-
 Bos taurus urate + H2O2
-
 ?

pH Optimum

EC Number pH Optimum Minimum pH Optimum Maximum Comment Organism
1.17.3.2 7.5
-
 assay at Rattus norvegicus
1.17.3.2 7.5
-
 assay at Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.17.3.2 0.000183
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(2-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000269
-
 pH 7.5, temperature not specified in the publication Bos taurus 2-[(4-methoxyphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000289
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(4-methoxyphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000326
-
 pH 7.5, temperature not specified in the publication Bos taurus 7-methyl-2-[(2-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000362
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 7-methyl-2-[(2-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000413
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(2-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000449
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(4-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000461
-
 pH 7.5, temperature not specified in the publication Bos taurus 2-[(4-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000555
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 7-methyl-2-(phenoxymethyl)-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00059
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(2-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000603
-
 pH 7.5, temperature not specified in the publication Bos taurus 2-[(2-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000623
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(4-chloro-3-methylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.000634
-
 pH 7.5, temperature not specified in the publication Bos taurus 2-[(4-chloro-3-methylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00073
-
 pH 7.5, temperature not specified in the publication Bos taurus allopurinol
1.17.3.2 0.000753
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus allopurinol
1.17.3.2 0.00102
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 7-methyl-2-[(4-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00103
-
 pH 7.5, temperature not specified in the publication Bos taurus 7-methyl-2-[(3-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00107
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 7-methyl-2-[(3-methylphenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00165
-
 pH 7.5, temperature not specified in the publication Bos taurus 2-[(2-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00176
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(2,4-dimethylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.0018
-
 pH 7.5, temperature not specified in the publication Bos taurus 2-[(2,4-dimethylphenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00198
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(3-fluorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00203
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 7-methyl-2-[(4-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.002501
-
 pH 7.5, temperature not specified in the publication Bos taurus 7-methyl-2-[(4-nitrophenoxy)methyl]-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00256
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(3-bromophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one
1.17.3.2 0.00618
-
 pH 7.5, temperature not specified in the publication Rattus norvegicus 2-[(3-chlorophenoxy)methyl]-7-methyl-5H-[1,3,4]thiadiazolo[3,2-a]pyrimidin-5-one

General Information

EC Number General Information Comment Organism
1.17.3.2 additional information elevated level of blood uric acid, hyperuricemia, is the underlying cause of gout, development of enzyme inhibitors more efficacious, than allopurinol, to treat gout and possibly against cardiovascular diseases, overview Rattus norvegicus
1.17.3.2 additional information elevated level of blood uric acid, hyperuricemia, is the underlying cause of gout, development of enzyme inhibitors more efficacious, than allopurinol, to treat gout and possibly against cardiovascular diseases, overview Bos taurus