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Literature summary for 1.1.1.21 extracted from

  • Chen, H.; Zhang, X.; Zhang, X.; Fan, Z.; Liu, W.; Lei, Y.; Zhu, C.; Ma, B.
    Dihydrobenzoxazinone derivatives as aldose reductase inhibitors with antioxidant activity (2020), Bioorg. Med. Chem., 28, 115699 .
    View publication on PubMed

Inhibitors

Inhibitors Comment Organism Structure
(2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid 7fold selectivity for ALR2 over ALR1 Homo sapiens
(2-oxo-8-phenyl-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
-
Homo sapiens
(2-oxo-8-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid 24fold selectivity for ALR2 over ALR1 Homo sapiens
epalrestat 26.7fold selectivity for ALR2 over ALR1 Homo sapiens
additional information use of dihydrobenzoxazinone derivatives as aldose reductase inhibitors. Most of the derivatives with styryl side chains exhibit good inhibitory activities and most of the compounds reveal powerful antioxidant activity Homo sapiens
[2-oxo-8-[(E)-2-phenylethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid 9fold selectivity for ALR2 over ALR1 Homo sapiens
[8-(4-formylphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
Homo sapiens
[8-(4-methoxyphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
Homo sapiens
[8-[(E)-2-(4-fluorophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid 25.7fold selectivity for ALR2 over ALR1 Homo sapiens
[8-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid 24fold selectivity for ALR2 over ALR1 Homo sapiens
[8-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid 60fold selectivity for ALR2 over ALR1 Homo sapiens
[8-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
Homo sapiens
[8-[(E)-2-(4-methylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
Homo sapiens
[8-[(E)-2-(4-nitrophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
Homo sapiens
[8-[(E)-2-(4-tert-butylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid 4fold selectivity for ALR2 over ALR1 Homo sapiens
[8-[(E)-2-([1,1'-biphenyl]-4-yl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens P15121
-
-

Synonyms

Synonyms Comment Organism
ALR2
-
Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.000045
-
pH 6.2, 30°C Homo sapiens epalrestat
0.000082
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-(4-hydroxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.000138
-
30°C, pH 6.2 Homo sapiens (2-oxo-8-[(E)-2-[4-(trifluoromethyl)phenyl]ethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
0.000167
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-(4-fluorophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.00017
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-(4-tert-butylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.000188
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-(4-hydroxy-3-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.000208
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-(4-methoxyphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.00022
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-(4-methylphenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.000262
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-(4-nitrophenyl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.000281
-
30°C, pH 6.2 Homo sapiens [8-[(E)-2-([1,1'-biphenyl]-4-yl)ethenyl]-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.000308
-
30°C, pH 6.2 Homo sapiens [2-oxo-8-[(E)-2-phenylethenyl]-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.000774
-
30°C, pH 6.2 Homo sapiens [8-(4-methoxyphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.00105
-
30°C, pH 6.2 Homo sapiens [8-(4-formylphenyl)-2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl]acetic acid
0.001932
-
30°C, pH 6.2 Homo sapiens (2-oxo-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid
0.00334
-
30°C, pH 6.2 Homo sapiens (2-oxo-8-phenyl-2,3-dihydro-4H-1,4-benzoxazin-4-yl)acetic acid