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Literature summary 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

EC Number Inhibitors Comment Organism Structure
1.1.1.21 (Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)-N-hydroxyacetamide
-
 Homo sapiens
1.1.1.21 (Z)-2-(5-biphenyl-4-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 18% inhibition at 0.0125 mM Homo sapiens
1.1.1.21 (Z)-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 32% inhibition at 0.0125 mM Homo sapiens
1.1.1.21 (Z)-2-(5-naphthalen-2-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 3% inhibition at 0.0125 mM Homo sapiens
1.1.1.21 (Z)-2-[2,4-dioxo-5-(3-phenoxybenzylidene)thiazolidin-3-yl]acetamide 8% inhibition at 0.0125 mM Homo sapiens
1.1.1.21 (Z)-2-[5-(3-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide 16% inhibition at 0.0125 mM Homo sapiens
1.1.1.21 (Z)-2-[5-(3-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide 10% inhibition at 0.0125 mM Homo sapiens
1.1.1.21 (Z)-2-[5-(4-benzyloxybenzylidene)-2,4-dioxothiazolidin-3-yl]-N-hydroxyacetamide
-
 Homo sapiens
1.1.1.21 (Z)-2-[5-(4-hydroxy-3-methoxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
-
 Homo sapiens
1.1.1.21 (Z)-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide 31% inhibition at 0.0125 mM Homo sapiens
1.1.1.21 (Z)-N-hydroxy-2-(5-naphthalen-1-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide
-
 Homo sapiens
1.1.1.21 (Z)-N-hydroxy-2-(5-naphthalen-2-ylmethylene-2,4-dioxothiazolidin-3-yl)acetamide 39% inhibition at 0.025 mM Homo sapiens
1.1.1.21 (Z)-N-hydroxy-2-[2,4-dioxo-5-(3-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
-
 Homo sapiens
1.1.1.21 (Z)-N-hydroxy-2-[2,4-dioxo-5-(4-phenoxybenzylidene)-thiazolidin-3-yl]acetamide
-
 Homo sapiens
1.1.1.21 (Z)-N-hydroxy-2-[5-(4-hydroxybenzylidene)-2,4-dioxothiazolidin-3-yl]acetamide
-
 Homo sapiens
1.1.1.21 epalrestat
-
 Homo sapiens
1.1.1.21 fidarestat
-
 Homo sapiens
1.1.1.21 lidorestat
-
 Homo sapiens
1.1.1.21 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
1.1.1.21 sorbinil
-
 Homo sapiens
1.1.1.21 Tolrestat
-
 Homo sapiens
1.1.1.21 zopolrestat
-
 Homo sapiens

Organism

EC Number Organism UniProt Comment Textmining
1.1.1.21 Homo sapiens P15121
-
-

Substrates and Products (Substrate)

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

Synonyms

EC Number Synonyms Comment Organism
1.1.1.21 aldose reductase
-
 Homo sapiens
1.1.1.21 ALR2
-
 Homo sapiens

Cofactor

EC Number Cofactor Comment Organism Structure
1.1.1.21 NADPH
-
 Homo sapiens

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.00141
-
 in 0.25 M potassium phosphate buffer pH 6.8, at 37°C Homo sapiens sorbinil
1.1.1.21 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
1.1.1.21 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
1.1.1.21 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
1.1.1.21 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
1.1.1.21 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
1.1.1.21 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
1.1.1.21 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