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Literature summary for 1.17.3.2 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

Inhibitors Comment Organism Structure
1-(3-(furan-2-yl)-4,5-dihydro-5-(pyridin-4-yl)pyrazol-1-yl)ethanone
-
Bos taurus
2,4-dichloro-6-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)phenol
-
Bos taurus
2-(3-phenyl-1H-pyrazol-5-yl)aniline
-
Bos taurus
2-(4-chlorophenyl)-5-(3,4-dimethoxyphenyl)-5,6-dihydropyrazolo[1,5-c]quinazoline
-
Bos taurus
2-methoxy-4-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)phenol
-
Bos taurus
2-phenylpyrazolo[1,5-c]quinazoline
-
Bos taurus
2-[3-(4-chlorophenyl)-1H-pyrazol-5-yl]aniline
-
Bos taurus
4-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)benzonitrile
-
Bos taurus
4-(2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl)phenol
-
Bos taurus
4-[2-(4-chlorophenyl)-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl]-2-methoxyphenol
-
Bos taurus
4-[2-(4-chlorophenyl)-5,6-dihydropyrazolo[1,5-c]quinazolin-5-yl]phenol
-
Bos taurus
5-(1H-indol-3-yl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
Bos taurus
5-(2-nitrophenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
Bos taurus
5-(3,4-dimethoxyphenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
Bos taurus
5-(3-nitrophenyl)-2-phenyl-5,6-dihydropyrazolo[1,5-c]quinazoline
-
Bos taurus
allopurinol 59.2% inhibition at 0.05 mM Bos taurus
curcumin
-
Bos taurus
febuxostat
-
Bos taurus
FYX-051
-
Bos taurus
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
N-(1-(3-bromophenyl)-3-(naphthalen-2-yl)-3-oxopropyl)acetamide
-
Bos taurus
Y-700
-
Bos taurus

Metals/Ions

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

Organism

Organism UniProt Comment Textmining
Bos taurus P80457
-
-

Source Tissue

Source Tissue Comment Organism Textmining
commercial preparation
-
Bos taurus
-
milk
-
Bos taurus
-

Temperature Optimum [°C]

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

pH Optimum

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

Cofactor

Cofactor Comment Organism Structure
molybdenum cofactor dioxothiomolybdenum cofactor Bos taurus

IC50 Value

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