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Literature summary extracted from

  • Papastavrou, N.; Chatzopoulou, M.; Ballekova, J.; Cappiello, M.; Moschini, R.; Balestri, F.; Patsilinakos, A.; Ragno, R.; Stefek, M.; Nicolaou, I.
    Enhancing activity and selectivity in a series of pyrrol-1-yl-1-hydroxypyrazole-based aldose reductase inhibitors The case of trifluoroacetylation (2017), Eur. J. Med. Chem., 130, 328-335 .
    View publication on PubMed

Inhibitors

EC Number Inhibitors Comment Organism Structure
1.1.1.21 1-[4-benzoyl-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]-2,2,2-trifluoroethan-1-one 413fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(3-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one 370fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one 468fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-phenoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one 190fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methanesulfonyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one 775fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one mixed-type inhibition Homo sapiens
1.1.1.21 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one 650fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 2,2,2-trifluoro-1-[4-(3-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one 339fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one mixed-type inhibition Homo sapiens
1.1.1.21 2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one 858fold selectivity for isoform ALR2 over ALR1 Rattus norvegicus
1.1.1.21 sorbinil
-
 Rattus norvegicus
1.1.1.21 Valproic acid
-
 Rattus norvegicus

Organism

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

Source Tissue

EC Number Source Tissue Comment Organism Textmining
1.1.1.21 kidney isoform ALR1 Rattus norvegicus
-
1.1.1.21 lens isoform ALR2 Rattus norvegicus
-

Substrates and Products (Substrate)

EC Number Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
1.1.1.21 4-hydroxynonenal + NADPH + H+
-
 Homo sapiens 4-hydroxynonanol + NADP+
-
 ?
1.1.1.21 DL-glyceraldehyde + NAD(P)H + H+
-
 Homo sapiens glycerol + NAD(P)+
-
 ?
1.1.1.21 L-idose + NADPH + H+
-
 Homo sapiens alditol + NADP+
-
 ?

IC50 Value

EC Number IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
1.1.1.21 0.000043
-
 pH 7.4, 37°C Rattus norvegicus 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methylsulfanyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
1.1.1.21 0.000064
-
 pH 7.4, 37°C Rattus norvegicus 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(3-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
1.1.1.21 0.000073
-
 pH 7.4, 37°C Rattus norvegicus 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-methoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
1.1.1.21 0.000078
-
 pH 7.4, 37°C Rattus norvegicus 2,2,2-trifluoro-1-[4-(4-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
1.1.1.21 0.000094
-
 pH 7.4, 37°C Rattus norvegicus 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-[4-(methanesulfonyl)benzoyl]-1H-pyrrol-2-yl]ethan-1-one
1.1.1.21 0.00014
-
 pH 7.4, 37°C Rattus norvegicus 2,2,2-trifluoro-1-[4-(3-fluorobenzoyl)-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]ethan-1-one
1.1.1.21 0.000242
-
 pH 7.4, 37°C Rattus norvegicus 1-[4-benzoyl-1-(1-hydroxy-1H-pyrazol-4-yl)-1H-pyrrol-2-yl]-2,2,2-trifluoroethan-1-one
1.1.1.21 0.00025
-
 isoform ALR2, pH 7.4, 37°C Rattus norvegicus sorbinil
1.1.1.21 0.00074
-
 pH 7.4, 37°C Rattus norvegicus 2,2,2-trifluoro-1-[1-(1-hydroxy-1H-pyrazol-4-yl)-4-(4-phenoxybenzoyl)-1H-pyrrol-2-yl]ethan-1-one
1.1.1.21 0.056
-
 isoform ALR1, pH 7.4, 37°C Rattus norvegicus Valproic acid