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Literature summary extracted from

  • Kumar, D.; Kaur, G.; Negi, A.; Kumar, S.; Singh, S.; Kumar, R.
    Synthesis and xanthine oxidase inhibitory activity of 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives (2014), Bioorg. Chem., 57, 57-64 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.17.3.2 1-(3-(furan-2-yl)-4,5-dihydro-5-(pyridin-4-yl)pyrazol-1-yl)ethanone
-
 Bos taurus
1.17.3.2 2,4-dichloro-6-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)phenol
-
 Bos taurus
1.17.3.2 2-(3-phenyl-1H-pyrazol-5-yl)aniline
-
 Bos taurus
1.17.3.2 2-(4-chlorophenyl)-5-(3,4-dimethoxyphenyl)-5,6-dihydropyrazolo[1,5-c]quinazoline
-
 Bos taurus
1.17.3.2 2-methoxy-4-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)phenol
-
 Bos taurus
1.17.3.2 2-phenylpyrazolo[1,5-c]quinazoline
-
 Bos taurus
1.17.3.2 2-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]aniline
-
 Bos taurus
1.17.3.2 4-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)benzonitrile
-
 Bos taurus
1.17.3.2 4-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)phenol
-
 Bos taurus
1.17.3.2 4-[2-(4-chlorophenyl)-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl]-2-methoxyphenol
-
 Bos taurus
1.17.3.2 4-[2-(4-chlorophenyl)-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl]phenol
-
 Bos taurus
1.17.3.2 5-(1H-indol-3-yl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
 Bos taurus
1.17.3.2 5-(2-nitrophenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
 Bos taurus
1.17.3.2 5-(3,4-dimethoxyphenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
 Bos taurus
1.17.3.2 5-(3-nitrophenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
 Bos taurus
1.17.3.2 allopurinol 59.2% inhibition at 0.05 mM Bos taurus
1.17.3.2 curcumin
-
 Bos taurus
1.17.3.2 febuxostat
-
 Bos taurus
1.17.3.2 FYX-051
-
 Bos taurus
1.17.3.2 additional information rational design, synthesis, and xanthine oxidase inhibitory activity of 5,6-dihydropyrazolo/pyrazolo[1,5-c]quinazoline derivatives, molecular docking into the enzyme's active site, structure activity relationship, overview. Mode of binding and important interactions such as hydrogen bonding, Pi-Pi stacking with amino acid residues like Ser876, Thr1010, Phen914, Phe1009, and Phe649 with close proximity to dioxothiomolybdenum Bos taurus
1.17.3.2 N-(1-(3-bromophenyl)-3-(naphthalen-2-yl)-3-oxopropyl)acetamide
-
 Bos taurus
1.17.3.2 Y-700
-
 Bos taurus

Metals/Ions

EC Number Metals/Ions Comment Organism Structure
1.17.3.2 Molybdenum in dioxothiomolybdenum cofactor Bos taurus

Organism

EC Number Organism UniProt Comment Textmining
1.17.3.2 Bos taurus P80457
-
-

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.17.3.2 commercial preparation
-
 Bos taurus
-
1.17.3.2 milk
-
 Bos taurus
-

Temperature Optimum [°C]

EC Number Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
1.17.3.2 22
-
 assay at room temperature Bos taurus

pH Optimum

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

Cofactor

EC Number Cofactor Comment Organism Structure
1.17.3.2 molybdenum cofactor dioxothiomolybdenum cofactor Bos taurus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.17.3.2 0.011
-
 pH 7.5, 22°C Bos taurus 2,4-dichloro-6-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)phenol
1.17.3.2 0.021
-
 pH 7.5, 22°C Bos taurus 5-(3-nitrophenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
1.17.3.2 0.0316
-
 pH 7.5, 22°C Bos taurus allopurinol
1.17.3.2 0.0417
-
 pH 7.5, 22°C Bos taurus 2-(3-phenyl-1H-pyrazol-5-yl)aniline
1.17.3.2 0.0437
-
 pH 7.5, 22°C Bos taurus 5-(3,4-dimethoxyphenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline