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Literature summary for 1.4.3.4 extracted from

  • Koc, G.?.; Tan, O.U.; Ucar, G.; Yildirim, E.; Erol, K.; Palaska, E.
    Synthesis and monoamine oxidase inhibitory activities of some 3-(4-fluorophenyl)-5-aryl-n-substituted-4,5-dihydro-(1H)-pyrazole-1-carbothioamide derivatives (2014), Drug Res., 64, 591-598 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
3-(4-fluorophenyl)-5-(2-naphthyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-5-(4-acetylaminophenyl)-N-phenyl-4,5-dihydro-1H -pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-5-(4-acetylaminophenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-5-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-5-(4-methoxyphenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-5-(4-methylphenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-N,5-diphenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-N-methyl-5-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-N-methyl-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
3-(4-fluorophenyl)-N-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
4-[1-(cyclopropylcarbamothioyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-5-yl]-N-methylbenzamide
-
Rattus norvegicus
4-[1-(ethylcarbamothioyl)-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazol-5-yl]-N-methylbenzamide
-
Rattus norvegicus
4-[3-(4-fluorophenyl)-1-(methylcarbamothioyl)-4,5-dihydro-1H-pyrazol-5-yl]-N-methylbenzamide
-
Rattus norvegicus
5-(4-bromophenyl)-3-(4-fluorophenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
5-(4-bromophenyl)-3-(4-fluorophenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
5-(4-bromophenyl)-N-cyclopropyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
5-(4-bromophenyl)-N-ethyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
5-(4-chlorophenyl)-3-(4-fluorophenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
5-(4-chlorophenyl)-3-(4-fluorophenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
5-(4-chlorophenyl)-N-cyclopropyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
5-(4-chlorophenyl)-N-ethyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
Clorgyline
-
Rattus norvegicus
N-cyclopropyl-3-(4-fluorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
N-cyclopropyl-3-(4-fluorophenyl)-5-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
N-cyclopropyl-3-(4-fluorophenyl)-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
N-cyclopropyl-3-(4-fluorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
N-ethyl-3-(4-fluorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
N-ethyl-3-(4-fluorophenyl)-5-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
N-ethyl-3-(4-fluorophenyl)-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
N-ethyl-3-(4-fluorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
-
Rattus norvegicus
Pargyline
-
Rattus norvegicus

Localization

Localization Comment Organism GeneOntology No. Textmining
mitochondrion
-
Rattus norvegicus 5739
-

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P19643
-
-
Rattus norvegicus P21396
-
-

Purification (Commentary)

Purification (Comment) Organism
-
Rattus norvegicus

Source Tissue

Source Tissue Comment Organism Textmining
liver
-
Rattus norvegicus
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
4-tyramine + H2O + O2
-
Rattus norvegicus (4-hydroxyphenyl)acetaldehyde + NH3 + H2O2
-
?
benzylamine + H2O + O2
-
Rattus norvegicus benzaldehyde + NH3 + H2O2
-
?

Synonyms

Synonyms Comment Organism
MAO-A
-
Rattus norvegicus
MAO-B
-
Rattus norvegicus
monoamine oxidase A
-
Rattus norvegicus
monoamine oxidase B
-
Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
FAD
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00172
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus Clorgyline
0.00625
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-3-(4-fluorophenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.00834
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-N-ethyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.01339
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 5-(4-bromophenyl)-3-(4-fluorophenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.0199
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-N-cyclopropyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.0299
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 5-(4-bromophenyl)-N-ethyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.03044
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 5-(4-bromophenyl)-N-cyclopropyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.03724
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-3-(4-fluorophenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.05522
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-5-(4-methoxyphenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.06128
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-N-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.08991
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus N-cyclopropyl-3-(4-fluorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.09045
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-N-methyl-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.09053
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.09821
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.09856
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-5-(2-naphthyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.0999
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus N-cyclopropyl-3-(4-fluorophenyl)-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.10077
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 4-[3-(4-fluorophenyl)-1-(methylcarbamothioyl)-4,5-dihydro-1H-pyrazol-5-yl]-N-methylbenzamide
0.1842
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.1859
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.19356
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-5-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.19723
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.19844
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-N-methyl-5-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.19886
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.20534
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-N-methyl-5-(4-methylphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.2459
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus N-cyclopropyl-3-(4-fluorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.25623
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-5-(4-methoxyphenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.26476
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus N-cyclopropyl-3-(4-fluorophenyl)-5-(4-methoxyphenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.39
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus Pargyline
0.43089
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus N-cyclopropyl-3-(4-fluorophenyl)-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.47004
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.47019
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-N-methyl-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.47021
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-N-methyl-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.47022
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-N-ethyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.47045
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 4-[3-(4-fluorophenyl)-1-(methylcarbamothioyl)-4,5-dihydro-1H-pyrazol-5-yl]-N-methylbenzamide
0.47066
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus N-ethyl-3-(4-fluorophenyl)-5-(naphthalen-2-yl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.47067
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 5-(4-bromophenyl)-N-cyclopropyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.48023
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 5-(4-bromophenyl)-N-ethyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.48055
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus N-cyclopropyl-3-(4-fluorophenyl)-5-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.4874
-
isoform MAO-A, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-5-(2-naphthyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.48882
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-3-(4-fluorophenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.49622
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 5-(4-bromophenyl)-3-(4-fluorophenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.50011
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-N-cyclopropyl-3-(4-fluorophenyl)-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.50023
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 5-(4-chlorophenyl)-3-(4-fluorophenyl)-N-methyl-4,5-dihydro-1H-pyrazole-1-carbothioamide
0.50045
-
isoform MAO-B, at pH 7.6 and 37°C Rattus norvegicus 3-(4-fluorophenyl)-5-(4-methoxyphenyl)-N-phenyl-4,5-dihydro-1H-pyrazole-1-carbothioamide