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Literature summary for 1.1.1.21 extracted from

  • Maccari, R.; Ottana, R.; Ciurleo, R.; Rakowitz, D.; Matuszczak, B.; Laggner, C.; Langer, T.
    Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives (2008), Bioorg. Med. Chem., 16, 5840-5852.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-N-hydroxyacetamide
-
Homo sapiens
(Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 18% inhibition at 0.0125 mM Homo sapiens
(Z)-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 32% inhibition at 0.0125 mM Homo sapiens
(Z)-2-(5-naphthalen-2-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 3% inhibition at 0.0125 mM Homo sapiens
(Z)-2-[2,4-dioxo-5-(3-phenoxybenzylidene)thiazolidin-3-yl]acetamide 8% inhibition at 0.0125 mM Homo sapiens
(Z)-2-[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide 16% inhibition at 0.0125 mM Homo sapiens
(Z)-2-[5-(3-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide 10% inhibition at 0.0125 mM Homo sapiens
(Z)-2-[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]-N-hydroxyacetamide
-
Homo sapiens
(Z)-2-[5-(4-hydroxy-3-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
-
Homo sapiens
(Z)-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide 31% inhibition at 0.0125 mM Homo sapiens
(Z)-N-hydroxy-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
-
Homo sapiens
(Z)-N-hydroxy-2-(5-naphthalen-2-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 39% inhibition at 0.025 mM Homo sapiens
(Z)-N-hydroxy-2-[2,4-dioxo-5-(3-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
-
Homo sapiens
(Z)-N-hydroxy-2-[2,4-dioxo-5-(4-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
-
Homo sapiens
(Z)-N-hydroxy-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
-
Homo sapiens
epalrestat
-
Homo sapiens
fidarestat
-
Homo sapiens
lidorestat
-
Homo sapiens
additional information not inhibited by (Z)-2-[2,4-dioxo-5-(4-phenoxybenzylidene)thiazolidin-3-yl]acetamide, (Z)-2-[5-(4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide, and (Z)-2-[5-(3-hydroxy-4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide Homo sapiens
sorbinil
-
Homo sapiens
Tolrestat
-
Homo sapiens
zopolrestat
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P15121
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
DL-glyceraldehyde + NADPH + H+
-
Homo sapiens glycerol + NADP+
-
?

Synonyms

Synonyms Comment Organism
aldose reductase
-
Homo sapiens
ALR2
-
Homo sapiens

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.00141
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens sorbinil
0.00179
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens (Z)-N-hydroxy-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
0.00367
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens (Z)-N-hydroxy-2-[2,4-dioxo-5-(4-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
0.0042
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens (Z)-N-hydroxy-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
0.00652
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens (Z)-2-[5-(4-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
0.00734
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens (Z)-2-[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]-N-hydroxyacetamide
0.0127
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens (Z)-N-hydroxy-2-[2,4-dioxo-5-(3-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
0.0203
-
in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens (Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-N-hydroxyacetamide