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Literature summary for 1.1.1.21 extracted from

  • Yang, Y.; Zhang, S.; Wu, B.; Ma, M.; Chen, X.; Qin, X.; He, M.; Hussain, S.; Jing, C.; Ma, B.; Zhu, C.
    An efficient synthesis of quinoxalinone derivatives as potent inhibitors of aldose reductase (2012), ChemMedChem, 7, 823-835.
    View publication on PubMed
Search for more literature for 1.1.1.21

Inhibitors

Inhibitors Comment Organism Structure
2-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-((2,4-difluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-((4-bromo-2-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
-
 Rattus norvegicus
2-(3-((4-bromophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-((4-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromo-2-fluorophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromo-2-fluorophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromo-2-fluorophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromo-2-fluorophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-bromophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(6-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(6-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(6-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(6-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(7-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(7-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(7-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
3,6,7-trichloroquinoxalin-2(1H)-one
-
 Rattus norvegicus
3,6-dichloroquinoxalin-2(1H)-one
-
 Rattus norvegicus
3,7-dichloroquinoxalin-2(1H)-one
-
 Rattus norvegicus
3-chloro-6-fluoroquinoxalin-2(1H)-one
-
 Rattus norvegicus
3-chloro-6-methylquinoxalin-2(1H)-one
-
 Rattus norvegicus
3-chloro-6-nitroquinoxalin-2(1H)-one
-
 Rattus norvegicus
3-chloro-7-fluoroquinoxalin-2(1H)-one
-
 Rattus norvegicus
3-chloro-7-methoxyquinoxalin-2(1H)-one
-
 Rattus norvegicus
3-chloro-7-methylquinoxalin-2(1H)-one
-
 Rattus norvegicus
3-chloroquinoxalin-2(1H)-one
-
 Rattus norvegicus
6,7-dichloro-3-(4-methylpiperazin-1-yl)quinoxalin-2(1H)-one
-
 Rattus norvegicus
6-bromo-3-chloroquinoxalin-2(1H)-one
-
 Rattus norvegicus
7-bromo-3-chloroquinoxalin-2(1H)-one
-
 Rattus norvegicus
epalrestat
-
 Rattus norvegicus
methyl 2-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-((2,4-difluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-((4-bromo-2-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-((4-bromophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-((4-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromo-2-fluorophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromo-2-fluorophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromo-2-fluorophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromo-2-fluorophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetat
-
 Rattus norvegicus
methyl 2-(3-(4-bromophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-bromophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(6-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(6-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(6-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(6-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(7-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(7-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(7-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
methyl 2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetate
-
 Rattus norvegicus
additional information synthesis of quinoxalinone derivatives as potent inhibitors of aldose reductase, Structure-activity relationship and molecular docking studies, overview Rattus norvegicus
rubrolide L
-
 Rattus norvegicus

Natural Substrates/ Products (Substrates)

Natural Substrates Organism Comment (Nat. Sub.) Natural Products Comment (Nat. Pro.) Rev. Reac.
D-glucose + NADPH + H+ Rattus norvegicus
-
 D-sorbitol + NADP+
-
 ?
D-glucose + NADPH + H+ Rattus norvegicus Wistar
-
 D-sorbitol + NADP+
-
 ?

Organism

Organism UniProt Comment Textmining
Rattus norvegicus
-
-
-
Rattus norvegicus Wistar
-
-
-

Substrates and Products (Substrate)

Substrates Comment Substrates Organism Products Comment (Products) Rev. Reac.
D-glucose + NADPH + H+
-
 Rattus norvegicus D-sorbitol + NADP+
-
 ?
D-glucose + NADPH + H+
-
 Rattus norvegicus Wistar D-sorbitol + NADP+
-
 ?

Synonyms

Synonyms Comment Organism
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
0.00000143
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus epalrestat
0.00000163
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(6-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.00000243
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.00000431
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(6-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000047
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(7-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.00000504
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(6-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000063
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(7-bromo-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000114
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000191
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(7-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000226
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromo-2-fluorophenoxy)-7-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000273
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000328
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.000033
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000356
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromo-2-fluorophenoxy)-7-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000382
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(6-bromo-3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000423
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(7-chloro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000435
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(7-bromo-3-(4-bromophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.000045
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromo-2-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000463
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromo-2-fluorophenoxy)-6-chloro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000493
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.00007
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(6-fluoro-3-(4-fluorophenoxy)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.0000748
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-(4-bromo-2-fluorophenoxy)-6-fluoro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.000124
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-((4-bromo-2-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)-acetic acid
0.00015
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-((4-bromophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.000494
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-((4-fluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.000987
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(2-oxo-3-((3,4,5-trifluorophenyl)amino)quinoxalin-1(2H)-yl)acetic acid
0.001204
-
 pH 6.2, 30°C, ALR2 Rattus norvegicus 2-(3-((2,4-difluorophenyl)amino)-2-oxoquinoxalin-1(2H)-yl)acetic acid

General Information

General Information Comment Organism
metabolism the enzyme catalyzes the first step in the polyol pathway of glucose metabolism Rattus norvegicus