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Literature summary for 1.4.3.4 extracted from

  • Prins, L.H.; Petzer, J.P.; Malan, S.F.
    Synthesis and in vitro evaluation of pteridine analogues as monoamine oxidase B and nitric oxide synthase inhibitors (2009), Bioorg. Med. Chem., 17, 7523-7530.
    View publication on PubMed
Search for more literature for 1.4.3.4

Inhibitors

Inhibitors Comment Organism Structure
1,3-dimethyl-6-phenyl-1H-pteridine-2,4-dione
-
 Papio sp.
6-(3-chlorophenyl)-1,3-dimethyl-1H-pteridine-2,4-dione
-
 Papio sp.
6-amino-1,3-dimethyl-5-([1-phenylmeth-(E)-ylidene]-amino)-1H-pyrimidine-2,4-dione
-
 Papio sp.
6-amino-1,3-dimethyl-5-[(E)-3-phenyl-prop-2-en-(E)-ylideneamino]-1H-pyrimidine-2,4-dione
-
 Papio sp.
6-amino-5-([1-(3-chlorophenyl)-meth-(E)-ylidene]-amino)-1,3-dimethyl-1H-pyrimidine-2,4-dione
-
 Papio sp.
6-amino-5-[(E)-3-(3-chloro-phenyl)-prop-2-en-(E)-ylideneamino]-1,3-dimethyl-1H-pyrimidine-2,4-dione
-
 Papio sp.
6-[(E)-2-(3-chloro-phenyl)-vinyl]-1,3-dimethyl-1H-pteridine-2,4-dione
-
 Papio sp.
6-[(E)-2-(3-chlorostyryl)]-1,3-dimethyl-1H-pteridine-2,4-dione
-
 Papio sp.
additional information potent reversible pteridine-2,4-dione analogue inhibitor development and synthesis, molecular modelling of MAO-B ligand binding, overview Papio sp.

KM Value [mM]

KM Value [mM] KM Value Maximum [mM] Substrate Comment Organism Structure
0.0683
-
 1-methyl-4-(1-methylpyrrol-2-yl)-1,2,3,6-tetrahydropyridine pH 7.4, 37°C Papio sp.

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
 Papio sp. 5739
-

Organism

Organism UniProt Comment Textmining
Papio sp.
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1-methyl-4-(1-methylpyrrol-2-yl)-1,2,3,6-tetrahydropyridine + H2O + O2 i.e. MMTP Papio sp. ?
-
 ?
additional information molecular modelling of MAO-B ligand binding, overview Papio sp. ?
-
 ?

Synonyms

Synonyms Comment Organism
MAO-B
-
 Papio sp.
monoamine oxidase B
-
 Papio sp.

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
 assay at Papio sp.

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
 assay at Papio sp.

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
additional information
-
 additional information sigmoidal dose–response curve of the initial rates of oxidation of MMTP versus the logarithm of concentration of inhibiton Papio sp.
0.181
-
 6-[(E)-2-(3-chlorostyryl)]-1,3-dimethyl-1H-pteridine-2,4-dione pH 7.4, 37°C Papio sp.
0.348
-
 6-amino-5-[(E)-3-(3-chloro-phenyl)-prop-2-en-(E)-ylideneamino]-1,3-dimethyl-1H-pyrimidine-2,4-dione pH 7.4, 37°C Papio sp.
2.823
-
 6-(3-chlorophenyl)-1,3-dimethyl-1H-pteridine-2,4-dione pH 7.4, 37°C Papio sp.
4.06
-
 6-amino-5-([1-(3-chlorophenyl)-meth-(E)-ylidene]-amino)-1,3-dimethyl-1H-pyrimidine-2,4-dione pH 7.4, 37°C Papio sp.
6.958
-
 6-amino-1,3-dimethyl-5-[(E)-3-phenyl-prop-2-en-(E)-ylideneamino]-1H-pyrimidine-2,4-dione pH 7.4, 37°C Papio sp.

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000314
-
 pH 7.4, 37°C Papio sp. 6-[(E)-2-(3-chloro-phenyl)-vinyl]-1,3-dimethyl-1H-pteridine-2,4-dione
0.000602
-
 pH 7.4, 37°C Papio sp. 6-amino-5-[(E)-3-(3-chloro-phenyl)-prop-2-en-(E)-ylideneamino]-1,3-dimethyl-1H-pyrimidine-2,4-dione
0.443
-
 pH 7.4, 37°C Papio sp. 1,3-dimethyl-6-phenyl-1H-pteridine-2,4-dione
0.467
-
 pH 7.4, 37°C Papio sp. 6-amino-1,3-dimethyl-5-([1-phenylmeth-(E)-ylidene]-amino)-1H-pyrimidine-2,4-dione
0.577
-
 pH 7.4, 37°C Papio sp. 6-amino-5-[(E)-3-(3-chloro-phenyl)-prop-2-en-(E)-ylideneamino]-1,3-dimethyl-1H-pyrimidine-2,4-dione
1.057
-
 pH 7.4, 37°C Papio sp. 6-[(E)-2-(3-chlorostyryl)]-1,3-dimethyl-1H-pteridine-2,4-dione
6.968
-
 pH 7.4, 37°C Papio sp. 6-amino-5-([1-(3-chlorophenyl)-meth-(E)-ylidene]-amino)-1,3-dimethyl-1H-pyrimidine-2,4-dione

General Information

General Information Comment Organism
physiological function MAO-Bis implicated in the pathology of neurodegenerative diseases Papio sp.