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Literature summary for 1.1.1.2 extracted from

  • Hussain, S.; Parveen, S.; Hao, X.; Zhang, S.; Wang, W.; Qin, X.; Yang, Y.; Chen, X.; Zhu, S.; Zhu, C.; Ma, B.
    Structure-activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors (2014), Eur. J. Med. Chem., 80, 383-392.
    View publication on PubMed
Search for more literature for 1.1.1.2

Inhibitors

Inhibitors Comment Organism Structure
1-(4-nitrobenzyl)-3-(4-(2-morpholinoethyl) piperazin-1-yl)quinoxalin-2(1H)-one 23% inhibition Rattus norvegicus
1-(4-nitrobenzyl)-3-(4-(3-(trifluoromethyl) phenyl)piperazin-1-yl) quinoxalin-2(1H)-one 43% inhibition Rattus norvegicus
1-(4-nitrobenzyl)-3-(4-(4-methoxyphenyl) piperazin-1-yl)quinoxalin-2(1H)-one 26% inhibition Rattus norvegicus
1-(4-nitrobenzyl)-3-(4-(pyrazin-2-yl) piperazin-1-yl)quinoxalin-2(1H)-one 24% inhibition Rattus norvegicus
1-(4-nitrobenzyl)-3-styrylquinoxalin-2(1H)-one 30% inhibition Rattus norvegicus
2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
2-(2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(6-chloro-3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
-
 Rattus norvegicus
2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid
-
 Rattus norvegicus
3-(4-fluorostyryl)-1-(4-nitrobenzyl) quinoxalin-2(1H)-one 24% inhibition Rattus norvegicus
3-(benzo[b] thiophen-3-yl)-1-(4-nitrobenzyl)quinoxalin-2(1H)-one 32% inhibition Rattus norvegicus
additional information structure-activity relationships study of quinoxalinone derivatives as aldose reductase inhibitors. Among them, N1-acetate derivatives have significant activity, molecular modeling and docking, overview. Both C3-phenethyl and C6-NO2 groups play an important role in enhancing the activity and selectivity of the quinoxalinone based inhibitors Rattus norvegicus
N-(tert-butyl)-3-(4-(4-nitrobenzyl)-3-oxo-3, 4-dihydroquinoxalin-2-yl) acryl amide 36% inhibition Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P51635
-
-
Rattus norvegicus Wistar P51635
-
-

Source Tissue

Source Tissue Comment Organism Textmining
additional information ALR1 is present in all tissues Rattus norvegicus
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
alcohol dehydrogenase [NADP(+)] UniProt Rattus norvegicus
aldehyde reductase
-
 Rattus norvegicus
ALR1
-
 Rattus norvegicus

Temperature Optimum [°C]

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

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
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
0.000143
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl) acetic acid
0.000283
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid
0.000362
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.00066
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(6-chloro-3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid
0.00082
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid
0.00114
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl) acetic acid
0.00143
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl) acetic acid
0.00186
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid
0.00388
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid
0.00753
-
 pH 7.2, 37°C, ALR1 Rattus norvegicus 2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl) acetic acid

General Information

General Information Comment Organism
physiological function ALR1 is present in all tissues and plays an important role in detoxification Rattus norvegicus