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Literature summary for 3.5.3.1 extracted from

  • da Silva, E.R.; Boechat, N.; Pinheiro, L.C.; Bastos, M.M.; Costa, C.C.; Bartholomeu, J.C.; da Costa, T.H.
    Novel selective inhibitor of Leishmania (Leishmania) amazonensis arginase (2015), Chem. Biol. Drug Des., 86, 969-978.
    View publication on PubMed
Search for more literature for 3.5.3.1

Inhibitors

Inhibitors Comment Organism Structure
2-(5-methyl-2-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)hydrazinecarbothioamide non-competitive inhibitor, 79% inhibition at 1 mM Leishmania amazonensis
5-methyl-2-(trifluoromethyl)-N-[3-(trifluoromethyl)-1H-1,2,4-triazol-5-yl][1,2,4]triazolo[1,5-a]pyrimidin-7-amine 57% inhibition at 1 mM Leishmania amazonensis
5-methyl-7-(1H-1,2,4-triazol-1-yl)-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidine 47% inhibition at 1 mM Leishmania amazonensis
5-methyl-7-(1H-pyrrol-1-yl)-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidine 38% inhibition at 1 mM Leishmania amazonensis
5-methyl-7-(4-trifluoromethylphenylamine)-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidine 52% inhibition at 1 mM Leishmania amazonensis
5-methyl-7-(pyrrolidin-1-yl)-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidine 10% inhibition at 1 mM Leishmania amazonensis
5-methyl-N-(naphthalen-2-yl)-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 29% inhibition at 1 mM Leishmania amazonensis
5-methyl-N-phenyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 1% inhibition at 1 mM Leishmania amazonensis
7-(4-chlorophenylamine)-5-methyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidine 42% inhibition at 1 mM Leishmania amazonensis
N-(2,6-difluorophenyl)-5-methyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 8% inhibition at 1 mM Leishmania amazonensis
N-(3,4-dichlorophenyl)-5-methyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 3% inhibition at 1 mM Leishmania amazonensis
N-(3,5-dichlorophenyl)-2,5-bis(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 47% inhibition at 1 mM Leishmania amazonensis
N-(3,5-dichlorophenyl)-2,5-dimethyl[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 23% inhibition at 1 mM Leishmania amazonensis
N-(3,5-dichlorophenyl)-5-methyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 71% inhibition at 1 mM Leishmania amazonensis
N-(3,5-dimethoxyphenyl)-5-methyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 39% inhibition at 1 mM Leishmania amazonensis
N-(3-chlorophenyl)-5-methyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 51% inhibition at 1 mM Leishmania amazonensis
N-(4-methoxyphenyl)-5-methyl-2-(trifluoromethyl)[1,2,4]triazolo[1,5-a]pyrimidin-7-amine 5% inhibition at 1 mM Leishmania amazonensis

Localization

Localization Comment Organism GeneOntology No. Textmining
glycosome
-
 Leishmania amazonensis 20015
-

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
L-arginine + H2O Leishmania amazonensis
-
 L-ornithine + urea
-
 ?

Organism

Organism UniProt Comment Textmining
Leishmania amazonensis O96394
-
-

Purification (Commentary)

Purification (Comment) Organism
-
 Leishmania amazonensis

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-arginine + H2O
-
 Leishmania amazonensis L-ornithine + urea
-
 ?

Synonyms

Synonyms Comment Organism
ARG
-
 Leishmania amazonensis

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.017
-
 2-(5-methyl-2-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)hydrazinecarbothioamide at pH 9.5 and 37°C Leishmania amazonensis

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.0165
-
 at pH 9.5 and 37°C Leishmania amazonensis 2-(5-methyl-2-(trifluoromethyl)-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)hydrazinecarbothioamide