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Literature summary extracted from

  • Gökhan-Kelekci, N.; Yabanoglu, S.; Küepeli, E.; Salgin, U.; Özgen, O.; Ucar, G.; Ye?ilada, E.; Kendi, E.; Yesilada, A.; Bilgin, A.A.
    A new therapeutic approach in Alzheimer disease: some novel pyrazole derivatives as dual MAO-B inhibitors and antiinflammatory analgesics (2007), Bioorg. Med. Chem., 15, 5775-5786.
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.4.3.4 1-N-allylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-A Rattus norvegicus
1.4.3.4 1-N-allylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-B Rattus norvegicus
1.4.3.4 1-N-allylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole non-selective inhibitor; non-selective inhibitor Rattus norvegicus
1.4.3.4 1-N-ethylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-A Rattus norvegicus
1.4.3.4 1-N-ethylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-B Rattus norvegicus
1.4.3.4 1-N-ethylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole non-selective inhibitor; non-selective inhibitor Rattus norvegicus
1.4.3.4 1-N-methylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-A Rattus norvegicus
1.4.3.4 1-N-methylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-B Rattus norvegicus
1.4.3.4 1-N-methylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole non-selective inhibitor; non-selective inhibitor Rattus norvegicus
1.4.3.4 1-N-phenylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-A Rattus norvegicus
1.4.3.4 1-N-phenylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole selective for MAO-B Rattus norvegicus
1.4.3.4 1-N-phenylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole non-selective inhibitor; non-selective inhibitor Rattus norvegicus
1.4.3.4 additional information monoamine oxidase-B inhibitors and antiinflammatory agents might be effective in treating AlzheimerÂ’s disease Rattus norvegicus
1.4.3.4 Pargyline
-
 Rattus norvegicus

Organism

EC Number Organism UniProt Comment Textmining
1.4.3.4 Rattus norvegicus P19643
-
-
1.4.3.4 Rattus norvegicus P21396
-
-

Purification (Commentary)

EC Number Purification (Comment) Organism
1.4.3.4
-
 Rattus norvegicus

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.4.3.4 liver
-
 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.4.3.4 p-tyramine + H2O + O2 MAO-B Rattus norvegicus (4-hydroxyphenyl)acetaldehyde + NH3 + H2O2
-
 ?

Synonyms

EC Number Synonyms Comment Organism
1.4.3.4 MAO-A
-
 Rattus norvegicus
1.4.3.4 MAO-B
-
 Rattus norvegicus

Ki Value [mM]

EC Number Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
1.4.3.4 0.0053
-
 Pargyline
-
 Rattus norvegicus
1.4.3.4 0.0125
-
 1-N-methylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, selective for MAO-B Rattus norvegicus
1.4.3.4 0.013
-
 1-N-methylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus
1.4.3.4 0.024
-
 1-N-ethylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, MAO-B, selective for MAO-B Rattus norvegicus
1.4.3.4 0.0269
-
 1-N-ethylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus
1.4.3.4 0.0333
-
 1-N-allylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus
1.4.3.4 0.0337
-
 1-N-allylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, MAO-B, selective for MAO-B Rattus norvegicus
1.4.3.4 0.0371
-
 1-N-phenylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, MAO-B, selective for MAO-B Rattus norvegicus
1.4.3.4 0.0608
-
 1-N-phenylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.4.3.4 0.029
-
 pH 7.6, 37°C, selective for MAO-B, no preincubation Rattus norvegicus 1-N-methylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.03
-
 pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus 1-N-methylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.0445
-
 pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus 1-N-ethylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.051
-
 pH 7.6, 37°C, selective for MAO-B, no preincubation Rattus norvegicus 1-N-ethylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.059
-
 pH 7.6, 37°C, selective for MAO-B, no preincubation Rattus norvegicus 1-N-allylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.066
-
 pH 7.6, 37°C, selective for MAO-B, no preincubation Rattus norvegicus 1-N-phenylthiocarbamoyl-3-(4-methoxyphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.0679
-
 pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus 1-N-allylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.098
-
 pH 7.6, 37°C, selective for MAO-A, no preincubation Rattus norvegicus 1-N-phenylthiocarbamoyl-3-(4-chlorophenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.302
-
 pH 7.6, 37°C, MAO-A, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-methylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.326
-
 pH 7.6, 37°C, MAO-A, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-phenylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.33
-
 pH 7.6, 37°C, MAO-A, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-ethylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.345
-
 pH 7.6, 37°C, MAO-B, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-phenylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.349
-
 pH 7.6, 37°C, MAO-B, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-methylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.366
-
 pH 7.6, 37°C, MAO-A, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-allylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.38
-
 pH 7.6, 37°C, MAO-B, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-ethylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole
1.4.3.4 0.39
-
 pH 7.6, 37°C, MAO-B, non-selective inhibitor, no preincubation Rattus norvegicus 1-N-allylthiocarbamoyl-3-(4-methylphenyl)-5-(2-pyrrolyl)-4,5-dihydro-(1H)-pyrazole