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Literature summary for 1.1.1.21 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 1.1.1.21

Inhibitors

Inhibitors Comment Organism Structure
1-(4-nitrobenzyl)-3-(4-(2-morpholinoethyl)piperazin-1-yl)quinoxalin-2(1H)-one
-
 Rattus norvegicus
1-(4-nitrobenzyl)-3-(4-(4-methoxyphenyl)piperazin-1-yl)quinoxalin-2(1H)-one
-
 Rattus norvegicus
1-(4-nitrobenzyl)-3-(4-(pyrazin-2-yl)piperazin-1-yl)quinoxalin-2(1H)-one}
-
 Rattus norvegicus
1-(4-nitrobenzyl)-3-styryl-quinoxalin-2(1H)-one
-
 Rattus norvegicus
2-(2-oxo-3-phenethylquinoxalin-1(2H)-yl)acetic acid 22% inhibition Rattus norvegicus
2-(2-oxo-3-styrylquinoxalin-1(2H)-yl)acetic acid 32% inhibition Rattus norvegicus
2-(3-(2,4-difluorophenylamino)-6-nitro-2-oxoquinoxalin-1(2H)-yl) acetic acid} 41% inhibition Rattus norvegicus
2-(3-(3-(tert-butylamino)-3-oxoprop-1-en-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 25% inhibition Rattus norvegicus
2-(3-(4-(4-methoxyphenyl) piperazin-1-yl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 48% inhibition Rattus norvegicus
2-(3-(4-fluorophenethyl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 40% inhibition Rattus norvegicus
2-(3-(4-fluorostyryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 47% inhibition Rattus norvegicus
2-(3-(4-fluorostyryl)-6-nitro-2-oxoquinoxalin-1(2H)-yl)acetic acid} 25% inhibition Rattus norvegicus
2-(6-chloro-3-(4-fluoro-styryl)-2-oxoquinoxalin-1(2H)-yl)acetic acid 25% inhibition Rattus norvegicus
2-(7-chloro-2-oxo-3-styrylquinoxalin-1(2H)-yl) acetic acid} 35% inhibition Rattus norvegicus
3-(4-fluorostyryl)-1-(4-nitrobenzyl)quinoxalin-2(1H)-one
-
 Rattus norvegicus
3-(benzo[b] thiophen-3-yl)-1-(4-nitrobenzylquinoxalin-2(1H)-one
-
 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-ylacryl amide
-
 Rattus norvegicus

Organism

Organism UniProt Comment Textmining
Rattus norvegicus P07943
-
-
Rattus norvegicus Wistar P07943
-
-

Substrates and Products (Substrate)

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

Synonyms

Synonyms Comment Organism
ALR2
-
 Rattus norvegicus

Temperature Optimum [°C]

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

pH Optimum

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

General Information

General Information Comment Organism
evolution aldose reductase (ALR2) is a member of aldo-keto reductase superfamily Rattus norvegicus