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Literature summary for 1.1.1.21 extracted from

  • Ramunno, A.; Cosconati, S.; Sartini, S.; Maglio, V.; Angiuoli, S.; La Pietra, V.; Di Maro, S.; Giustiniano, M.; La Motta, C.; Da Settimo, F.; Marinelli, L.; Novellino, E.
    Progresses in the pursuit of aldose reductase inhibitors: the structure-based lead optimization step (2012), Eur. J. Med. Chem., 51, 216-226.
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
epalrestat
-
Rattus norvegicus
fidarestat
-
Rattus norvegicus
additional information inhibitor development, synthesis and molecular docking, overview Rattus norvegicus
N-(2-phenylethyl)-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-(2-phenylethyl)-N-[(3-nitrophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-(2-phenylethyl)-N-[(4-bromophenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-(2-phenylethyl)-N-[(4-chlorophenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-(2-phenylethyl)-N-[(4-fluorophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-(2-phenylethyl)-N-[(4-methylphenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-(2-phenylethyl)-N-[(4-nitrophenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-(2-phenylethyl)-N-[(4-trifluoromethylphenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-benzyl-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-benzyl-N-[(2-naphthalenyl)sulfonyl]glycine
-
Rattus norvegicus
N-benzyl-N-[(3-nitrophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-benzyl-N-[(4-bromophenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-benzyl-N-[(4-chlorophenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-benzyl-N-[(4-fluorophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-benzyl-N-[(4-methylphenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-benzyl-N-[(4-nitrophenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-benzyl-N-[(4-trifluoromethylphenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(1,10-biphenyl)-4-sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(1-naphthalenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(2-naphthalenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(3-nitrophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(4-bromophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(4-chlorophenyl)sulfonyl]glycine no inhibition of ALR1 Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(4-fluorophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(4-nitrophenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1 naphthalenyl)sulfonyl]glycine
-
Rattus norvegicus
N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1-naphthalenyl)sulfonyl]glycine
-
Rattus norvegicus
S12728 inhibitor of ALR2, but no inhibition of ALR1 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-
Rattus norvegicus Sprague-Dawley
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-glucuronate + NADPH substrate of aldehyde reductase ALR1 Rattus norvegicus ? + NADP+
-
?
D-glucuronate + NADPH substrate of aldehyde reductase ALR1 Rattus norvegicus Sprague-Dawley ? + NADP+
-
?
DL-glyceraldehyde + NADPH substrate of aldose reductase ALR2 Rattus norvegicus glycerol + NADP+
-
?
DL-glyceraldehyde + NADPH substrate of aldose reductase ALR2 Rattus norvegicus Sprague-Dawley glycerol + NADP+
-
?

Synonyms

Synonyms Comment Organism
aldehyde reductase
-
Rattus norvegicus
aldose reductase
-
Rattus norvegicus
ALR1
-
Rattus norvegicus
ALR2
-
Rattus norvegicus

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
30
-
assay at, ALR2 Rattus norvegicus
37
-
assay at, ALR1 Rattus norvegicus

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
6.2
-
assay at, ALR2 Rattus norvegicus
7.2
-
assay at, ALR1 Rattus norvegicus

Cofactor

Cofactor Comment Organism Structure
NADPH
-
Rattus norvegicus

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000431
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(3-nitrophenyl)sulfonyl]glycine
0.0011
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(3-nitrophenyl)sulfonyl]glycine
0.0012
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(1,10-biphenyl)-4-sulfonyl]glycine
0.0022
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0036
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(4-bromophenyl)sulfonyl]glycine
0.00427
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(2-naphthalenyl)sulfonyl]glycine
0.0046
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-bromophenyl)sulfonyl]glycine
0.0055
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0055
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(3-nitrophenyl)sulfonyl]glycine
0.0059
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(2-naphthalenyl)sulfonyl]glycine
0.0065
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(2-naphthalenyl)sulfonyl]glycine
0.0076
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(3-nitrophenyl)sulfonyl]glycine
0.0083
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-benzyl-N-[(2-naphthalenyl)sulfonyl]glycine
0.0104
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-(2-phenylethyl)-N-[(3-nitrophenyl)sulfonyl]glycine
0.0108
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-fluorophenyl)sulfonyl]glycine
0.0119
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-nitrophenyl)sulfonyl]glycine
0.0124
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(1-naphthalenyl)sulfonyl]glycine
0.0133
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1 naphthalenyl)sulfonyl]glycine
0.0147
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(1-naphthalenyl)sulfonyl]glycine
0.016
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(5-dimethylamino-1-naphthalenyl)sulfonyl]glycine
0.017
-
pH 6.2, 30°C, ALR2 Rattus norvegicus epalrestat
0.0173
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(4-nitrophenyl)sulfonyl]glycine
0.018
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0188
-
pH 6.2, 30°C, ALR2 Rattus norvegicus S12728
0.021
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(4-nitrophenyl)sulfonyl]glycine
0.0224
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-chlorophenyl)sulfonyl]glycine
0.0234
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(4-chlorophenyl)sulfonyl]glycine
0.0248
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(4-methylphenyl)sulfonyl]glycine
0.0265
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(1,10-biphenyl)-4-sulfonyl]glycine
0.029
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(4-fluorophenyl)sulfonyl]glycine
0.0339
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-benzyl-N-[(4-fluorophenyl)sulfonyl]glycine
0.0454
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(4-chlorophenyl)sulfonyl]glycine
0.0471
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(4-fluorophenyl)sulfonyl]glycine
0.0525
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
0.0576
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0578
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-bromophenyl)sulfonyl]glycine
0.0612
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-fluorophenyl)sulfonyl]glycine
0.0659
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-(2-phenylethyl)-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0683
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
0.0704
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(4-bromophenyl)sulfonyl]glycine
0.0732
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
0.0745
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-(2-phenylethyl)-N-[(4-fluorophenyl)sulfonyl]glycine
0.0747
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-benzyl-N-[(4-trifluoromethylphenyl)sulfonyl]glycine
0.0804
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-benzyl-N-[(2-fluoro-4-bromophenyl)sulfonyl]glycine
0.0847
-
pH 6.2, 30°C, ALR2 Rattus norvegicus N-(2-phenylethyl)-N-[(4-methylphenyl)sulfonyl]glycine
0.0847
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-[2-(2-thienyl)ethyl]-N-[(4-nitrophenyl)sulfonyl]glycine
0.0881
-
pH 7.2, 37°C, ALR1 Rattus norvegicus N-benzyl-N-[(3-nitrophenyl)sulfonyl]glycine
0.094
-
pH 7.2, 37°C, ALR1 Rattus norvegicus epalrestat