Any feedback?
Please rate this page
(literature.php)
(0/150)

BRENDA support

Literature summary for 3.4.22.B69 extracted from

  • Sharma, R.K.; Younis, Y.; Mugumbate, G.; Njoroge, M.; Gut, J.; Rosenthal, P.J.; Chibale, K.
    Synthesis and structure-activity-relationship studies of thiazolidinediones as antiplasmodial inhibitors of the Plasmodium falciparum cysteine protease falcipain-2 (2015), Eur. J. Med. Chem., 90, 507-518.
    View publication on PubMed
Search for more literature for 3.4.22.B69

Inhibitors

Inhibitors Comment Organism Structure
(5Z)-3-(2,4-difluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-3-(3-methoxybenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-3-(4-fluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-3-(4-methylbenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-3-benzyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-3-ethyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-3-methyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-3-[4-(trifluoromethyl)benzyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
(5Z)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-adamantyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-(4-cyanophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-(4-methoxyphenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-cyclohexylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-methylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenoxypiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dichlorobenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dimethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,5-ditrifluoromethylbenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-bromobenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-chlorobenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3,4-difluorobenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-carboxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-fluorobenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-isopropylbenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methoxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methylbenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-chlorobenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-fluorobenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methoxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methylbenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethylbenzylidene)
-
 Plasmodium falciparum
3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-benzylidene-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(4-pyridylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
3-[2-oxo-2-(piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
-
 Plasmodium falciparum
artesunate
-
 Plasmodium falciparum
Chloroquine
-
 Plasmodium falciparum
E-64
-
 Plasmodium falciparum
[(5Z)-2,4-dioxo-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidin-3-yl]acetic acid
-
 Plasmodium falciparum

Organism

Organism UniProt Comment Textmining
Plasmodium falciparum
-
-
-
Plasmodium falciparum W2
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-Val-Leu-Arg-7-amido-4-methylcoumarin + H2O
-
 Plasmodium falciparum D-Val-Leu-Arg + 7-amino-4-methylcoumarin
-
 ?
D-Val-Leu-Arg-7-amido-4-methylcoumarin + H2O
-
 Plasmodium falciparum W2 D-Val-Leu-Arg + 7-amino-4-methylcoumarin
-
 ?

Synonyms

Synonyms Comment Organism
FP-2
-
 Plasmodium falciparum

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000047
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum E-64
0.01123
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-(4-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.01224
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-(4-cyanophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.01264
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-(2-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.01344
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
0.0158
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-chlorobenzylidene)1,3-thiazolidine-2,4-dione
0.01625
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-(3-chlorophenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.01804
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-trifluoromethylbenzylidene)
0.02388
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-bromobenzylidene)1,3-thiazolidine-2,4-dione
0.02389
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-isopropylbenzylidene)1,3-thiazolidine-2,4-dione
0.02908
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-(2,4-difluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.02908
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-adamantyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.03325
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-fluorobenzylidene)1,3-thiazolidine-2,4-dione
0.03375
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenoxypiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.03528
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,5-ditrifluoromethylbenzylidene)1,3-thiazolidine-2,4-dione
0.03528
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
0.03624
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-benzyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.0388
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-benzylidene-1,3-thiazolidine-2,4-dione
0.04335
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-(4-methylbenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.04497
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-trifluoromethoxybenzylidene)1,3-thiazolidine-2,4-dione
0.04533
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methylbenzylidene)1,3-thiazolidine-2,4-dione
0.04571
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methylbenzylidene)1,3-thiazolidine-2,4-dione
0.04784
-
 in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dimethoxybenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-methoxybenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-methoxybenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-fluorobenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3,4-difluorobenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(4-chlorobenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(2,4-dichlorobenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-phenylpiperazin-1-yl)ethyl]-5-(3-carboxybenzylidene)1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum [(5Z)-2,4-dioxo-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidin-3-yl]acetic acid
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-methylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-cyclohexylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-pyridylpiperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum 3-[2-oxo-2-(4-(4-methoxyphenyl)piperazin-1-yl)ethyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-methyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-ethyl-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-(4-fluorobenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-[4-(trifluoromethyl)benzyl]-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione
0.05
-
 IC50 above 0.05 mM, in 100 mM sodium acetate, pH 5.5, at 22°C Plasmodium falciparum (5Z)-3-(3-methoxybenzyl)-5-(2,4,6-trimethoxybenzylidene)-1,3-thiazolidine-2,4-dione