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Literature summary for 3.4.11.20 extracted from

  • Mistry, S.N.; Drinkwater, N.; Ruggeri, C.; Sivaraman, K.K.; Loganathan, S.; Fletcher, S.; Drag, M.; Paiardini, A.; Avery, V.M.; Scammells, P.J.; McGowan, S.
    Two-pronged attack: dual inhibition of Plasmodium falciparum M1 and M17 metalloaminopeptidases by a novel series of hydroxamic acid-based inhibitors (2014), J. Med. Chem., 57, 9168-9183.
    View publication on PubMed
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Inhibitors

Inhibitors Comment Organism Structure
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide highly effective against the malaria parasites, IC50 values of 233 nM; highly effective against the malaria parasites, IC50 values of 233 nM Plasmodium falciparum
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide highly effective against the malaria parasites, IC50 values of 283 nM; highly effective against the malaria parasites, IC50 values of 283 nM Plasmodium falciparum
N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM; most effective inhibitor of isoform M1 and one of the more potent inhibitors of isoform M17 tested, the most effective compound against 3D7 malaria parasites, with an IC50 of 227 nM Plasmodium falciparum
tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives; compound shows good in vitro inhibitory properties, but IC50 for parasite growth is only 783 nM, suggesting that compounds substituted with the N-Boc group are either less capable of cellular penetration or less stable than the corresponding N-acyl derivatives Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum O96935
-
-
Plasmodium falciparum Q8IL11
-
-
Plasmodium falciparum isolate FcB1/Columbia O96935
-
-

Synonyms

Synonyms Comment Organism
M1 aminopeptidase
-
 Plasmodium falciparum
M17 aminopeptidase
-
 Plasmodium falciparum

Ki Value [mM]

Ki Value [mM] Ki Value maximum [mM] Inhibitor Comment Organism Structure
0.000011
-
 N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide pH 8.0, 37°C Plasmodium falciparum
0.000014
-
 N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide pH 8.0, 37°C Plasmodium falciparum
0.000028
-
 N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide pH 8.0, 37°C Plasmodium falciparum
0.00003
-
 tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate pH 8.0, 37°C Plasmodium falciparum
0.0007
-
 N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-pivalamide pH 8.0, 37°C Plasmodium falciparum
0.0008
-
 tert-butyl (1-(4-(1H-Pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)carbamate pH 8.0, 37°C Plasmodium falciparum
0.0055
-
 N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-3-aminobenzamide pH 8.0, 37°C Plasmodium falciparum
0.0074
-
 N-(1-(4-(1H-pyrazol-1-yl)phenyl)-2-(hydroxyamino)-2-oxoethyl)-4-aminobenzamide pH 8.0, 37°C Plasmodium falciparum