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Literature summary for 3.4.11.20 extracted from

  • Flipo, M.; Beghyn, T.; Leroux, V.; Florent, I.; Deprez, B.P.; Deprez-Poulain, R.F.
    Novel selective inhibitors of the zinc plasmodial aminopeptidase PfA-M1 as potential antimalarial agents (2007), J. Med. Chem., 50, 1322-1334.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid (4-phenyl-butyl)-amide
-
Plasmodium falciparum
1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid 4-fluoro-benzylamide
-
Plasmodium falciparum
2-(4-benzyl-piperidine-1-carbonyl)-4-methyl-pentanoic acid hydroxyamide
-
Plasmodium falciparum
2-benzyl-3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-propionamide
-
Plasmodium falciparum
2-benzyl-3-(4-benzyl-piperazin-1-yl)-N-hydroxy-3-oxo-propionamide
-
Plasmodium falciparum
2-benzyl-3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-propionamide
-
Plasmodium falciparum
2-benzyl-N-(2,2-diphenyl-ethyl)-N'-hydroxy-malonamide
-
Plasmodium falciparum
2-benzyl-N-(4-chloro-benzyl)-N'-hydroxy-malonamide
-
Plasmodium falciparum
2-benzyl-N-(4-fluoro-benzyl)-N'-hydroxy-malonamide
-
Plasmodium falciparum
2-benzyl-N-biphenyl-3-ylmethyl-N'-hydroxy-malonamide
-
Plasmodium falciparum
2-benzyl-N-hydroxy-N'-(2-methyl-benzyl)-malonamide
-
Plasmodium falciparum
2-benzyl-N-hydroxy-N'-(3-phenoxy-benzyl)-malonamide
-
Plasmodium falciparum
2-benzyl-N-hydroxy-N'-(3-phenyl-propyl)-malonamide
-
Plasmodium falciparum
2-benzyl-N-hydroxy-N'-(4-phenyl-butyl)-malonamide
-
Plasmodium falciparum
2-benzyl-N-hydroxy-N'-indan-2-yl-malonamide
-
Plasmodium falciparum
2-benzyl-N-hydroxy-N'-naphthalen-1-ylmethyl-malonamide
-
Plasmodium falciparum
2-benzyl-N-hydroxy-N'-phenethyl-malonamide
-
Plasmodium falciparum
2N-dibenzyl-N'-hydroxy-malonamide
-
Plasmodium falciparum
3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-2-(3-phenoxy-benzyl)-propionamide
-
Plasmodium falciparum
3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-2-(3-phenoxybenzyl)-propionamide
-
Plasmodium falciparum
N-(4-chloro-benzyl)-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
-
Plasmodium falciparum
N-(4-chloro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
-
Plasmodium falciparum
N-(4-fluoro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
-
Plasmodium falciparum
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(E)-ylidene]-malonamide
-
Plasmodium falciparum
N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
-
Plasmodium falciparum
N-benzyl-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
-
Plasmodium falciparum
N-benzyl-N'-hydroxy-2-isobutyl-malonamide in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(3-phenyl-propyl)-malonamide
-
Plasmodium falciparum
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-phenyl-butyl)-malonamide
-
Plasmodium falciparum
N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-trifluoromethyl-benzyl)-malonamide
-
Plasmodium falciparum
N-hydroxy-2-isobutyl-N'-(1,2,3,4-tetrahydro-naphthalen-1-yl)-malonamide
-
Plasmodium falciparum
N-hydroxy-2-isobutyl-N'-(3-phenoxy-benzyl)-malonamide
-
Plasmodium falciparum
N-hydroxy-2-isobutyl-N'-(3-phenyl-propyl)-malonamide
-
Plasmodium falciparum
N-hydroxy-2-isobutyl-N'-(4-phenyl-butyl)-malonamide
-
Plasmodium falciparum
N-hydroxy-2-isobutyl-N'-naphthalen-1-ylmethyl-malonamide
-
Plasmodium falciparum
N-hydroxy-2-isobutyl-N'-phenethyl-malonamide
-
Plasmodium falciparum
N-hydroxy-N'-(4-phenyl-butyl)-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-
Plasmodium falciparum FcB1
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
L-Leu-p-nitroanilide + H2O
-
Plasmodium falciparum L-Leu + p-nitroaniline
-
?
L-Leu-p-nitroanilide + H2O
-
Plasmodium falciparum FcB1 L-Leu + p-nitroaniline
-
?

Synonyms

Synonyms Comment Organism
PfA-M1 belongs to the M1 family and displays a strict aminopeptidase activity at pH 7.4 and a broad substrate spectrum Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000006
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
0.000013
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-N'-(4-phenyl-butyl)-2-[1-phenyl-meth-(Z)-ylidene]-malonamide
0.000027
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-(4-fluoro-benzyl)-N'-hydroxy-malonamide
0.000041
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-hydroxy-N'-(2-methyl-benzyl)-malonamide
0.000045
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-isobutyl-N'-(3-phenoxy-benzyl)-malonamide
0.000046
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-hydroxy-N'-(4-phenyl-butyl)-malonamide
0.000091
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-isobutyl-N'-naphthalen-1-ylmethyl-malonamide
0.000107
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-hydroxy-N'-naphthalen-1-ylmethyl-malonamide
0.000109
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-isobutyl-N'-(1,2,3,4-tetrahydro-naphthalen-1-yl)-malonamide
0.000125
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2N-dibenzyl-N'-hydroxy-malonamide
0.000125
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-hydroxy-N'-(3-phenyl-propyl)-malonamide
0.00013
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-(4-chloro-benzyl)-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
0.000164
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-benzyl-N'-hydroxy-2-(3-phenoxy-benzyl)-malonamide
0.00017
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-(4-chloro-benzyl)-N'-hydroxy-malonamide
0.000206
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-propionamide
0.000225
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-phenyl-butyl)-malonamide
0.000231
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-(3-phenoxy-benzyl)-N'-(4-trifluoromethyl-benzyl)-malonamide
0.000248
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 3-(4-benzyl-piperidin-1-yl)-N-hydroxy-3-oxo-2-(3-phenoxybenzyl)-propionamide
0.000253
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-propionamide
0.00033
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-(4-fluoro-benzyl)-N'-hydroxy-2-[1-phenyl-meth-(E)-ylidene]-malonamide
0.000406
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-(4-benzyl-piperidine-1-carbonyl)-4-methyl-pentanoic acid hydroxyamide
0.000495
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-benzyl-N'-hydroxy-2-isobutyl-malonamide
0.000527
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-(3-phenoxy-benzyl)-N'-(3-phenyl-propyl)-malonamide
0.00079
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-isobutyl-N'-(3-phenyl-propyl)-malonamide
0.000885
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-isobutyl-N'-phenethyl-malonamide
0.000904
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-(4-chloro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
0.000966
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 3-(3,4-dihydro-1H-isoquinolin-2-yl)-N-hydroxy-3-oxo-2-(3-phenoxy-benzyl)-propionamide
0.001011
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-hydroxy-N'-phenethyl-malonamide
0.001149
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-hydroxy-2-isobutyl-N'-(4-phenyl-butyl)-malonamide
0.001168
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-biphenyl-3-ylmethyl-N'-hydroxy-malonamide
0.00176
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-3-(4-benzyl-piperazin-1-yl)-N-hydroxy-3-oxo-propionamide
0.001931
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-hydroxy-N'-indan-2-yl-malonamide
0.002515
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-hydroxy-N'-(3-phenoxy-benzyl)-malonamide
0.003896
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum N-(4-fluoro-benzyl)-N'-hydroxy-2-isobutyl-malonamide
0.005363
-
in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 2-benzyl-N-(2,2-diphenyl-ethyl)-N'-hydroxy-malonamide
0.01
-
IC50 above 0.01 mM, in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid 4-fluoro-benzylamide
0.01
-
IC50 above 0.01 mM, in Tris-HCl buffer (25 mM, pH 7.4), at 25┬░C Plasmodium falciparum 1-hydroxy-2-oxo-1,2-dihydro-quinoline-3-carboxylic acid (4-phenyl-butyl)-amide