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(10-benzyl-3,4-dioxo-3,4-dihydro[1,2,4]triazino[4,3-a]benzimidazol-2(10H)-yl)acetic acid
-
(2R)-2,3-dihydroxypropanamide
-
(2R)-2-hydroxypropanamide
-
(2R,3S,4R,5R)-2,3,4,5,6-pentahydroxyhexanamide
-
(2R,3S,4S)-2,3,4,5-tetrahydroxypentanamide
-
(2S)-2,3-dihydroxypropanamide
-
(2S,3R,4R)-2,3,4,5-tetrahydroxypentanamide
-
(2S,3S)-2,3,4-trihydroxybutanamide
-
(4-benzyl-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl)acetic acid
-
(4S)-6-fluoro-2,3-dihydro-2'H,5'H-spiro[1-benzopyran-4,4'-imidazolidine]-2',5'-dione
-
1'-(4-bromophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-chlorophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-methoxyphenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-methylphenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(4-nitrophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(9,10-dioxo-9,10-dihydroanthracen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
1'-(naphthalen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
2-(3,4-dihydroxyphenyl)-3,5,7-trihydroxy-4H-1-benzopyran-4-one
-
2-(3,4-dihydroxyphenyl)-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(3,4-dihydroxyphenyl)-6-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(3,4-dihydroxyphenyl)-9-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(3,4-dimethoxyphenyl)-6-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(4-hydroxy-3-methoxyphenyl)-7-methyl-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-(6-nitro-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl)propanoic acid
-
2-benzyl-1,3,3-trioxo-2,3-dihydro-1H-3lambda~6~-naphtho[1,2-d][1,2]thiazole-4-carboxylic acid
-
2-phenyl-4H-pyrido[1,2-a]pyrimidin-4-one
-
2-[(3,4-dihydroxyphenyl)methyl]-6-hydroxy-4H-pyrido[1,2-a]pyrimidin-4-one
-
3'-(4-bromophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(4-chlorophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(4-methoxyphenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(4-methylphenylsulfonyl)spiro[fluorene-9,50-imidazolidine]-2',4'-dione
-
3'-(4-nitrophenylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(9,10-dioxo-9,10-dihydroanthracen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3'-(naphthalen-2-ylsulfonyl)spiro[fluorene-9,5'-imidazolidine]-2',4'-dione
-
3-(4-nitro-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl)propanoic acid
-
3-(6-acetamido-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl)propanoic acid
-
3-[6-(3-methylbutanamido)-1,1,3-trioxo-1,3-dihydro-2H-1lambda~6~,2-benzothiazol-2-yl]propanoic acid
-
4-[(3-nitrophenyl)methyl]-7-oxo-4,7-dihydropyrazolo[1,5-a]pyrimidine-6-carboxylic acid
-
6-hydroxy-2-phenyl-4H-pyrido[1,2-a]pyrimidin-4-one
-
[(2E)-2-[2-(carboxymethyl)hydrazinylidene]-3-[[4-(trifluoromethyl)phenyl]methyl]-2,3-dihydro-1H-benzimidazol-1-yl](oxo)acetic acid
-
[(5Z)-5-[(2E)-2-methyl-3-phenylprop-2-en-1-ylidene]-4-oxo-2-sulfanylidene-1,3-thiazolidin-3-yl]acetic acid
-
[3,4-dioxo-10-[[4-(trifluoromethyl)phenyl]methyl]-3,4-dihydro[1,2,4]triazino[4,3-a]benzimidazol-2(10H)-yl]acetic acid
-
[3-[(4-chlorophenyl)methyl]-1,2,4-oxadiazol-5-yl]acetic acid
-
[5-methyl-7-oxo-4-(2-phenylethyl)-4,7-dihydropyrazolo[1,5-a]pyrimidin-6-yl]acetic acid
-
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid
-
IC50: 0.0017 mM
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid methyl ester
-
15% inhibition of ALR2 at 0.05 mM
(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-acetic acid
-
IC50: 0.00026 mM
(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-acetic acid methyl ester
-
35% inhibition of ALR2 at 0.05 mM
(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetic acid
-
IC50: 0.00017 mM
(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetic acid methyl ester
-
12% inhibition of ALR2 at 0.05 mM
(Z)-5-(naphthalen-1-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
52% inhibition at 0.025 mM
(Z)-5-(naphthalen-2-ylmethylidene)-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
59% inhibition at 0.025 mM
(Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(3-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
64% inhibition at 0.025 mM
(Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
-
(Z)-5-[(4-phenylphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
45% inhibition at 0.025 mM
1,5-bis(3,4-dihydroxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0034 mM
1,5-bis(3,5-di-tert-butyl-4-hydroxyphenyl)-1,4-pentadiene-3-one
-
31.0% inhibition at 0.1 mM
1,5-bis(4-hydroxy-3,5-dimethoxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0253 mM
1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0359 mM
1,5-bis(4-hydroxyphenyl)-1,4-pentadiene-3-one
-
IC50: 0.0331 mM
2,5-bis(3,4-dihydroxybenzylidene)cyclopentanone
-
IC50: 0.0026 mM
2,5-bis(3,5-di-tert-butyl-4-hydroxybenzylidene)cyclopentanone
-
38.2% inhibition at 0.1 mM
2,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclopentanone
-
IC50: 0.0208 mM
2,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclopentanone
-
IC50: 0.0234 mM
2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone
-
IC50: 0.0258 mM
2,5-bis(4-hydroxybenzylidene)cyclopentanone
-
IC50: 0.0274 mM
2,6-bis(3,4-dihydroxybenzylidene)cyclohexanone
-
IC50: 0.0029 mM
2,6-bis(3,5-di-tert-butyl-4-hydroxybenzylidene)cyclohexanone
-
35.8% inhibition at 0.1 mM
2,6-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclohexanone
-
IC50: 0.021 mM
2,6-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclohexanone
-
IC50: 0.0249 mM
2,6-bis(4-hydroxy-3-methoxybenzylidene)cyclohexanone
-
IC50: 0.0264 mM
2,6-bis(4-hydroxybenzylidene)cyclohexanone
-
IC50: 0.0275 mM
2-[5-fluoro-2-methyl-1-p-(methylsulphinyl)benzylidine]indene-3-acetic acid
-
non-competitive
3,5-bis(3,4-dihydroxybenzylidene)-4-piperidone
-
IC50: 0.0049 mM
3,5-bis(3,5-di-tert-butyl-4-hydroxybenzylidene)-4-piperidone
-
29.2% inhibition at 0.1 mM
3,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)-4-piperidone
-
IC50: 0.0208 mM
3,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)-4-piperidone
-
IC50: 0.0223 mM
3,5-bis(4-hydroxy-3-methoxybenzylidene)-4-piperidone
-
IC50: 0.0299 mM
3,5-bis(4-hydroxyphenyl)-4-piperidone
-
IC50: 0.0311 mM
4-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-2-butenoic acid
-
21% inhibition of ALR2 at 0.05 mM
4-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-2-butenoic acid methyl ester
-
6% inhibition of ALR2 at 0.05 mM
4-[2,4-dioxo-5-(3-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid
-
19% inhibition of ALR2 at 0.05 mM
4-[2,4-dioxo-5-(3-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid methyl ester
-
25% inhibition of ALR2 at 0.05 mM
4-[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid
-
57% inhibition of ALR2 at 0.05 mM
4-[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]-2-butenoic acid methyl ester
-
23% inhibition of ALR2 at 0.05 mM
4-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]-2-butenoic acid
-
IC50: 0.0042 mM
5-(3-aminobenzylidene)-2,4-thiazolidinedione
-
IC50: 0.0202 mM
5-(3-hydroxybenzylidene)-2,4-thiazolidinedione
-
IC50: 0.0107 mM
5-(3-methoxybenzyl)-2,4-thiazolidinedione
-
16% inhibition of ALR2 at 0.05 mM
5-(3-nitrobenzylidene)-2,4-thiazolidinedione
-
21% inhibition of ALR2 at 0.05 mM
5-(3-phenoxybenzyl)-2,4-thiazolidinedione
-
IC50: 0.0789 mM
5-(4-aminobenzylidene)-2,4-thiazolidinedione
-
44% inhibition of ALR2 at 0.05 mM
5-(4-benzyloxybenzyl)-2,4-thiazolidinedione
-
IC50: 0.0314 mM
5-(4-benzyloxybenzylidene)-2,4-thiazolidinedione
-
10% inhibition of ALR2 at 0.05 mM
5-(4-hydroxybenzylidene)-2,4-thiazolidinedione
-
IC50: 0.009 mM
5-(4-methoxybenzyl)-2,4-thiazolidinedione
-
21% inhibition of ALR2 at 0.05 mM
5-(4-nitrobenzylidene)-2,4-thiazolidinedione
-
37% inhibition of ALR2 at 0.05 mM
5-(4-phenoxybenzyl)-2,4-thiazolidinedione
-
IC50: 0.0404 mM
5-biphenyl-4-ylmethyl-2,4-thiazolidinedione
-
IC50: 0.0658 mM
5-biphenyl-4-ylmethylene-2,4-thiazolidinedione
-
20% inhibition of ALR2 at 0.05 mM
5-naphthalen-1-ylmethylene-2,4-thiazolidinedione
-
IC50: 0.0107 mM
8-bromo-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid
-
4fold decreased inhibitory potency compared to the nonsubstituted parent compound
8-chloro-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid
-
4fold decreased inhibitory potency compared to the nonsubstituted parent compound
8-methyl-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid
-
2fold decreased inhibitory potency compared to the nonsubstituted parent compound
bisdemethoxycurcumin
-
i.e. 1,7-bis(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0137 mM
Ca2+
-
10 mM inhibits complex formation of ALR 2 with alpha-crystallin
Cl-
-
at high ionic strength
Cu2+
-
oxidative inactivation of ALR2, ratio Cu2+ to enzyme of 2:1, precipitation of the enzyme occurs at higher Cu2+ concentration, alpha-crystallin stabilizes the enzyme and protects against inactivation and precipitation by Cu2+ with higher efficiency at 37°C compared to 25°C, overview
CuCl2
-
addition of dithiothreitol or 2-mercaptoethanol recovers activity
curcumin
-
i.e. 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0068 mM
demethoxycurcumin
-
i.e. 1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0159 mM
disodium 4,6-dioxo-10-propyl-4H,6H-pyranol[3,2-g-]-quinoline-2,8-dicarboxylate
-
non-competitive
glyceraldehyde
-
substrate inhibition
malondialdehyde
-
at concentration above 0.8 mM substrate inhibition
Mg2+
-
10 mM inhibits complex formation of ALR 2 with alpha-crystallin, induces ALR 2 aggregation and precipitation
p-Carboxybenzaldehyde
-
substrate inhibition at higher concentration
p-hydroxymercuribenzoate
-
-
p-nitrobenzaldehyde
-
at concentration above 2 mM substrate inhibition
ponalrestat
-
IC50: 80 nM
quercetin
-
IC50: 0.0376 mM
sorbitol
-
competitive inhibition with NADP+ and glucose
sulfhydryl inhibitors
-
-
-
thienocinnolinone alkanoic acid derivatives
-
i.e. 8-halogen-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid derivatives, synthesis and inhibitory potency, IC50 as low as 0.0314 mM, the length of the N2 alkanoic chain strongly influences the inhibitory activity, overview
-
zofenoprilat-glutathione disulfide
-
the enzyme is specifically S-thionylated and inactivated by ZSSG, a homodisulfide formed by GSH and zofenoprilat, an angiotensin-converting enzyme inhibitor carrying a thiol group, which is more stable than glutathione, optimization, overview
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid
-
IC50: 0.0010 mM
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester
-
26% inhibition of ALR2 at 0.05 mM
[2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid
-
IC50: 0.0028 mM
[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetic acid
-
IC50: 0.00082 mM
[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetic acid methyl ester
-
33% inhibition of ALR2 at 0.05 mM
[5-(3-aminobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
IC50: 0.039 mM
[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.00066 mM
[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
43% inhibition of ALR2 at 0.05 mM
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.0030 mM
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
IC50: 0.0211 mM
[5-(3-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
-
IC50: 0.00049 mM
[5-(3-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
22% inhibition of ALR2 at 0.05 mM
[5-(4-aminobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
25% inhibition of ALR2 at 0.05 mM
[5-(4-benzyloxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
24% inhibition of ALR2 at 0.05 mM
[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.00028 mM
[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
12% inhibition of ALR2 at 0.05 mM
[5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.0021 mM
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.00015 mM
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
IC50: 0.0062 mM
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
-
IC50: 0.0011 mM
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
-
24% inhibition of ALR2 at 0.05 mM
[5-(4-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
-
IC50: 0.0012 mM
[5-(4-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
-
8% inhibition of ALR2 at 0.05 mM
NADP+
![hide entries hide](./images/icon_minus_white.png)
-
-
NADP+
-
competitve to NADPH
sorbinil
![hide entries hide](./images/icon_minus_white.png)
-
-
sorbinil
-
IC50: 0.0011 mM
sorbinil
-
IC50: 0.0034 mM
additional information
![hide entries hide](./images/icon_minus_white.png)
partial nonclassical competitive inhibition is exerted by the aldose hemiacetal on the reduction of the free aldehyde, aldose reductase modulation by hemiacetals, negative cooperative behavior of AR acting on L-idose, mechanism of inhibition, kinetic modelling, nonclassical competitive model, detailed overview
-
additional information
-
partial nonclassical competitive inhibition is exerted by the aldose hemiacetal on the reduction of the free aldehyde, aldose reductase modulation by hemiacetals, negative cooperative behavior of AR acting on L-idose, mechanism of inhibition, kinetic modelling, nonclassical competitive model, detailed overview
-
additional information
synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5-imidazolidine]-2,4-diones, analysis of the Kador-Sharpless model for minimal pharmacophoric requirements for an aldose reductase inhibitor, and superposition of target molecules on a hypoglycemic pharmacophoric model and a aldose reductase pharmacophoric model, overview. Molecular dynamics simulations and inhibitor binding model. Effects of the compounds on diabetic BALB/c mice
-
additional information
-
high ionic strength inhibits the enzyme to a higher extent when NADPH instead of NADH is used as a cofactor
-
additional information
-
scarcely inhibitory: sorbinil
-
additional information
-
molecular modelling, enzyme docking at the active site of the enzyme, structure-activity relationships of 5-arylidene-2,4-thiazolidinediones, an additional aromatic ring or an H-bond donor group on the 5-benzylidene ring enhance ALR2 inhibitory potency, the presence of a carboxylic anionic chain on N-3 is important, and the length of the carboxylic chain is critical, overview, no inhibition by 5b 4-[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]-2-butenoic acid methyl ester
-
additional information
-
no inhibition by 3,5-bis(3,4-dimethoxybenzylidene)-4-piperidone, 1,5-bis(3,4-dimethoxyphenyl)-1,4-pentadiene-3-one, 2,5-bis(3,4-dimethoxybenzylidene)cyclopentanone, and 2,6-bis(3,4-dimethoxybenzylidene)cyclohexanone, at 0.1 mM
-
additional information
-
poor inhibition by [2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid methyl ester
-
additional information
-
synthesis and evaluation of 2,4-thiazolidinedione inhibitors, structure-activity relationships, overview. No inhibition by (Z)-5-[(4-benzyloxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
-
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0.0017
(5-biphenyl-4-ylmethyl-2,4-dioxothiazolidin-3-yl)acetic acid
Bos taurus
-
IC50: 0.0017 mM
0.00026
(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-acetic acid
Bos taurus
-
IC50: 0.00026 mM
0.00017
(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetic acid
Bos taurus
-
IC50: 0.00017 mM
0.0123
(Z)-5-[(3-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0233
(Z)-5-[(3-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.003
(Z)-5-[(4-hydroxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0174
(Z)-5-[(4-methoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0083
(Z)-5-[(4-phenoxyphenyl)methylidene]-3-(3,3,3-trifluoro-2-oxopropyl)-2,4-thiazolidinedione
Bos taurus
-
pH 6.8, 37°C
0.0034
1,5-bis(3,4-dihydroxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0034 mM
0.0253
1,5-bis(4-hydroxy-3,5-dimethoxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0253 mM
0.0359
1,5-bis(4-hydroxy-3-methoxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0359 mM
0.0331
1,5-bis(4-hydroxyphenyl)-1,4-pentadiene-3-one
Bos taurus
-
IC50: 0.0331 mM
0.0026
2,5-bis(3,4-dihydroxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0026 mM
0.0208
2,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0208 mM
0.0234
2,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0234 mM
0.0258
2,5-bis(4-hydroxy-3-methoxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0258 mM
0.0274
2,5-bis(4-hydroxybenzylidene)cyclopentanone
Bos taurus
-
IC50: 0.0274 mM
0.0029
2,6-bis(3,4-dihydroxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0029 mM
0.021
2,6-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.021 mM
0.0249
2,6-bis(4-hydroxy-3,5-dimethoxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0249 mM
0.0264
2,6-bis(4-hydroxy-3-methoxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0264 mM
0.0275
2,6-bis(4-hydroxybenzylidene)cyclohexanone
Bos taurus
-
IC50: 0.0275 mM
0.0049
3,5-bis(3,4-dihydroxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0049 mM
0.0208
3,5-bis(3-bromo-4-hydroxy-5-methoxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0208 mM
0.0223
3,5-bis(4-hydroxy-3,5-dimethoxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0223 mM
0.0299
3,5-bis(4-hydroxy-3-methoxybenzylidene)-4-piperidone
Bos taurus
-
IC50: 0.0299 mM
0.0311
3,5-bis(4-hydroxyphenyl)-4-piperidone
Bos taurus
-
IC50: 0.0311 mM
0.0042
4-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]-2-butenoic acid
Bos taurus
-
IC50: 0.0042 mM
0.0202
5-(3-aminobenzylidene)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0202 mM
0.0107
5-(3-hydroxybenzylidene)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0107 mM
0.0789
5-(3-phenoxybenzyl)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0789 mM
0.0314
5-(4-benzyloxybenzyl)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0314 mM
0.009
5-(4-hydroxybenzylidene)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.009 mM
0.0404
5-(4-phenoxybenzyl)-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0404 mM
0.0658
5-biphenyl-4-ylmethyl-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0658 mM
0.0107
5-naphthalen-1-ylmethylene-2,4-thiazolidinedione
Bos taurus
-
IC50: 0.0107 mM
0.0137
bisdemethoxycurcumin
Bos taurus
-
i.e. 1,7-bis(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0137 mM
0.0068
curcumin
Bos taurus
-
i.e. 1,7-bis(4-hydroxy-3-methoxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0068 mM
0.0159
demethoxycurcumin
Bos taurus
-
i.e. 1-(4-hydroxy-3-methoxyphenyl)-7-(4-hydroxyphenyl)-1,6-heptadiene-3,5-dione, extracted from Curcuma longa roots, IC50: 0.0159 mM
0.00008
ponalrestat
Bos taurus
-
IC50: 80 nM
0.0376
quercetin
Bos taurus
-
IC50: 0.0376 mM
0.0314
thienocinnolinone alkanoic acid derivatives
Bos taurus
-
i.e. 8-halogen-4,4a-5,6-tetrahydrothieno[2,3-h]cinnolinone-N2-alkanoic acid derivatives, synthesis and inhibitory potency, IC50 as low as 0.0314 mM, the length of the N2 alkanoic chain strongly influences the inhibitory activity, overview
-
0.001
[2,4-dioxo-5-(3-phenoxybenzyl)thiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0010 mM
0.0028
[2,4-dioxo-5-(4-phenoxybenzyl)thiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0028 mM
0.00082
[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00082 mM
0.039
[5-(3-aminobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid methyl ester
Bos taurus
-
IC50: 0.039 mM
0.00066
[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00066 mM
0.003
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0030 mM
0.0211
[5-(3-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
Bos taurus
-
IC50: 0.0211 mM
0.00049
[5-(3-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
Bos taurus
-
IC50: 0.00049 mM
0.00028
[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00028 mM
0.0021
[5-(4-hydroxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0021 mM
0.00015
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.00015 mM
0.0062
[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetic acid methyl ester
Bos taurus
-
IC50: 0.0062 mM
0.0011
[5-(4-methoxybenzyl)-2,4-dioxothiazolidin-3-yl]acetic acid
Bos taurus
-
IC50: 0.0011 mM
0.0012
[5-(4-nitrobenzylidene)-2,4-dioxothiazolidin-3-yl]-acetic acid
Bos taurus
-
IC50: 0.0012 mM
additional information
additional information
Bos taurus
inhibition kinetics and thermodynamics, overview
-
0.0011
sorbinil
![hide entries hide](./images/icon_minus_white.png)
Bos taurus
-
IC50: 0.0011 mM
0.002
sorbinil
Bos taurus
-
pH 6.8, 37°C
0.0034
sorbinil
Bos taurus
-
IC50: 0.0034 mM
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Sheaff, C.M.; Doughty, C.C.
Physical and kinetic properties of homogenous bovine lens aldose reductase
J. Biol. Chem.
251
2696-2702
1976
Bos taurus
brenda
Cromlish, J.A.; Flynn, T.G.
Purification and characterization of two aldose reductase isoenzymes from rabbit muscle
J. Biol. Chem.
258
3416-3424
1983
Bos taurus, Oryctolagus cuniculus, Rattus norvegicus, Sus scrofa
brenda
Dons, R.F.; Doughty, C.C.
Isolation and characterization of aldose reductase from calf brain
Biochim. Biophys. Acta
452
1-12
1976
Bos taurus
brenda
Hayman, S.; Kinoshita, J.H.
Isolation and properties of lens aldose reductase
J. Biol. Chem.
240
877-882
1965
Bos taurus
brenda
Attwood, M.A.; Doughty, C.C.
Purification and properties of calf liver aldose reductase
Biochim. Biophys. Acta
370
358-368
1974
Bos taurus
brenda
Halder, A.B.; Crabbe, M.J.C.
Bovine lens aldehyde reductase (aldose reductase)
Biochem. J.
219
33-39
1984
Bos taurus
brenda
Ryle, C.M.; Dowling, T.G.; Tipton, K.F.
Purification and properties of low-KM aldehyde reductase from ox brain
Biochim. Biophys. Acta
791
155-163
1984
Bos taurus
brenda
Ryle, C.M.; Tipton, K.F.
Kinetic studies with low-KM aldehyde reductase from ox brain
Biochem. J.
227
621-627
1985
Bos taurus
brenda
Marini, I.; Bucchioni, L.; Voltarelli, M.; Del Corso, A.; Mura, U.
Alpha-crystallin-like molecular chaperone against the thermal denaturation of lens aldose reductase: the effect of divalent metal ions
Biochem. Biophys. Res. Commun.
212
413-420
1995
Bos taurus
brenda
Cecconi, I.; Scaloni, A.; Rastelli, G.; Moroni, M.; Vilardo, P.G.; Costantino, L.; Cappiello, M.; Garland, D.; Carper, D.; Petrash, J.M.; Del Corso, A.; Mura, U.
Oxidative modification of aldose reductase induced by copper ion. Definition of the metal-protein interaction mechanism
J. Biol. Chem.
277
42017-42027
2002
Bos taurus, Homo sapiens, Rattus norvegicus
brenda
Dal Monte, M.; Del Corso, A.; Moschini, R.; Cappiello, M.; Amodeo, P.; Mura, U.
Zofenoprilat-glutathione mixed disulfide as a specific S-thiolating agent of bovine lens aldose reductase
Antioxid. Redox Signal.
7
841-848
2005
Bos taurus
brenda
Moschini, R.; Marini, I.; Malerba, M.; Cappiello, M.; Del Corso, A.; Mura, U.
Chaperone-like activity of alpha-crystallin toward aldose reductase oxidatively stressed by copper ion
Arch. Biochem. Biophys.
453
13-17
2006
Bos taurus
brenda
Du, Z.Y.; Bao, Y.D.; Liu, Z.; Qiao, W.; Ma, L.; Huang, Z.S.; Gu, L.Q.; Chan, A.S.
Curcumin analogs as potent aldose reductase inhibitors
Arch. Pharm.
339
123-128
2006
Bos taurus
brenda
Maccari, R.; Ottana, R.; Curinga, C.; Vigorita, M.G.; Rakowitz, D.; Steindl, T.; Langer, T.
Structure-activity relationships and molecular modelling of 5-arylidene-2,4-thiazolidinediones active as aldose reductase inhibitors
Bioorg. Med. Chem.
13
2809-2823
2005
Bos taurus
brenda
Rakowitz, D.; Maccari, R.; Ottana, R.; Vigorita, M.G.
In vitro aldose reductase inhibitory activity of 5-benzyl-2,4-thiazolidinediones
Bioorg. Med. Chem.
14
567-574
2006
Bos taurus
brenda
Pau, A.; Asproni, B.; Murineddu, G.; Boatto, G.; Grella, G.E.; Rakowitz, D.; Costantino, L.; Pinna, G.A.
Thienocinnolinone alkanoic acid derivatives as aldose reductase inhibitors
Med. Chem.
2
39-45
2006
Bos taurus
brenda
Maccari, R.; Ciurleo, R.; Giglio, M.; Cappiello, M.; Moschini, R.; Corso, A.D.; Mura, U.; Ottana, R.
Identification of new non-carboxylic acid containing inhibitors of aldose reductase
Bioorg. Med. Chem.
18
4049-4055
2010
Bos taurus
brenda
Balestri, F.; Cappiello, M.; Moschini, R.; Rotondo, R.; Buggiani, I.; Pelosi, P.; Mura, U.; Del-Corso, A.
L-Idose: an attractive substrate alternative to D-glucose for measuring aldose reductase activity
Biochem. Biophys. Res. Commun.
456
891-895
2015
Homo sapiens (P15121), Homo sapiens, Bos taurus (P16116), Bos taurus
brenda
Balestri, F.; Cappiello, M.; Moschini, R.; Rotondo, R.; Abate, M.; Del-Corso, A.; Mura, U.
Modulation of aldose reductase activity by aldose hemiacetals
Biochim. Biophys. Acta
1850
2329-2339
2015
Homo sapiens (P15121), Homo sapiens, Bos taurus (P16116), Bos taurus
brenda
Iqbal, Z.; Hameed, S.; Ali, S.; Tehseen, Y.; Shahid, M.; Iqbal, J.
Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5-imidazolidine]-2,4-diones
Eur. J. Med. Chem.
98
127-138
2015
Bos taurus (P16116)
brenda
Del-Corso, A.; Balestri, F.; Di Bugno, E.; Moschini, R.; Cappiello, M.; Sartini, S.; La-Motta, C.; Da-Settimo, F.; Mura, U.
A new approach to control the enigmatic activity of aldose reductase
PLoS ONE
8
e74076
2013
Bos taurus (P16116)
brenda