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Literature summary for 3.4.23.39 extracted from

  • Faeh, C.; Hardegger, L.A.; Baitsch, L.; Schweizer, W.B.; Meyer, S.; Bur, D.; Diederich, F.
    New organofluorine building blocks: inhibition of the malarial aspartic proteases plasmepsin II and IV by alicyclic alpha,alpha-difluoroketone hydrates (2009), Org. Biomol. Chem., 7, 3947-3957.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(1RS) 3,3-difluoro-N-[2-(2-naphthyl)ethyl]-4-oxo-N-(4-pentylphenyl)cyclohexanecarboxamide
-
Plasmodium falciparum
(1RS,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
-
Plasmodium falciparum
(1SR,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
-
Plasmodium falciparum
2-(2-naphthyl)-N-(4-pentylphenyl)-N-piperidin-4-ylacetamide hydrochloride
-
Plasmodium falciparum
N-(4-hexylphenyl)-2-(2-naphthyl)-N-piperidin-4-ylacetamide hydrochloride
-
Plasmodium falciparum
N-([(1RS)-3,3-difluoro-4-oxocyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-([(1RS)-3,3-difluoro-4-oxocyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-([(1RS,4RS)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-([(1RS,4SR)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-([(1SR,4RS)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-([(1SR,4SR)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-[(1SR,3RS)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-[(1SR,3SR)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
-
Plasmodium falciparum
N-[4,4-difluoro-3-oxocyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)-acetamide
-
Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-

Synonyms

Synonyms Comment Organism
PM II
-
Plasmodium falciparum

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Plasmodium falciparum

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
5
-
assay at Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.007
-
pH 5.0, 37°C Plasmodium falciparum N-([(1RS)-3,3-difluoro-4-oxocyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.01
-
pH 5.0, 37°C Plasmodium falciparum (1RS) 3,3-difluoro-N-[2-(2-naphthyl)ethyl]-4-oxo-N-(4-pentylphenyl)cyclohexanecarboxamide
0.013
-
pH 5.0, 37°C Plasmodium falciparum N-(4-hexylphenyl)-2-(2-naphthyl)-N-piperidin-4-ylacetamide hydrochloride
0.016
-
pH 5.0, 37°C Plasmodium falciparum N-([(1RS,4SR)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.019
-
pH 5.0, 37°C Plasmodium falciparum N-([(1RS,4RS)-3,3-difluoro-4-hydroxycyclohexyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.019
-
pH 5.0, 37°C Plasmodium falciparum 2-(2-naphthyl)-N-(4-pentylphenyl)-N-piperidin-4-ylacetamide hydrochloride
0.02
-
pH 5.0, 37°C Plasmodium falciparum N-[(1SR,3SR)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.024
-
pH 5.0, 37°C Plasmodium falciparum N-[(1SR,3RS)-4,4-difluoro-3-hydroxycyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.024
-
pH 5.0, 37°C Plasmodium falciparum N-[4,4-difluoro-3-oxocyclohexyl]-2-(2-naphthyl)-N-(4-pentylphenyl)-acetamide
0.038
-
pH 5.0, 37°C Plasmodium falciparum (1SR,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
0.043
-
pH 5.0, 37°C Plasmodium falciparum (1RS,4RS)-3,3-difluoro-4-hydroxy-N-[2-(2-naphthyl)ethyl]-N(4-pentylphenyl)cyclohexanecarboxamide
0.1
-
value above, pH 5.0, 37°C Plasmodium falciparum N-([(1SR,4SR)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.1
-
value above, pH 5.0, 37°C Plasmodium falciparum N-([(1SR,4RS)-3,3-difluoro-4-hydroxycyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide
0.1
-
value above, pH 5.0, 37°C Plasmodium falciparum N-([(1RS)-3,3-difluoro-4-oxocyclopentyl]methyl)-2-(2-naphthyl)-N-(4-pentylphenyl)acetamide