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Literature summary for 1.1.1.21 extracted from

  • Rao, V.R.; Muthenna, P.; Shankaraiah, G.; Akileshwari, C.; Babu, K.H.; Suresh, G.; Babu, K.S.; Chandra Kumar, R.S.; Prasad, K.R.; Yadav, P.A.; Petrash, J.M.; Reddy, G.B.; Rao, J.M.
    Synthesis and biological evaluation of new piplartine analogues as potent aldose reductase inhibitors (ARIs) (2012), Eur. J. Med. Chem., 57, 344-361.
    View publication on PubMedView publication on EuropePMC

Inhibitors

Inhibitors Comment Organism Structure
(5-methylIndoleDs)1-(3-(3,4,5-trimethoxyphenyl)-3-(5-methyl-1H-indol-3-yl)propanoyl)-4-(5-methyl-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
(5-methylIndoleMs)1-(3-(3,4,5-trimethoxyphenyl)-3-(5-methyl-1H-indol-3-yl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(1,3-diphenyl-1H-pyrazol-4-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(2,5-dimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)piperidin-2-one
-
Homo sapiens
(E)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)pyrrolidin-2-one
-
Homo sapiens
(E)-1-(3-(3-(trifluoromethyl)phenyl)acryloyl)-5,6-dihydropyridin-2(1)-one
-
Homo sapiens
(E)-1-(3-(3-methyl-1-phenyl-1H-pyrazol-4-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(3-phenoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(4-bromophenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(4-chlorophenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(benzo[d][1,3]dioxol-5-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(furan-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(naphthalen-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(pyridin-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-(thiophen-2-yl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(3-mesitylacryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-1-(4-benzylpiperazin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
Homo sapiens
(E)-1-(4-methylpiperazin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
Homo sapiens
(E)-1-(4-phenylpiperazin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
Homo sapiens
(E)-1-(piperidin-1-yl)-3-(3,4,5-trimethoxyphenyl) prop-2-en-1-one
-
Homo sapiens
(E)-1-(pyrrolidin-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
-
Homo sapiens
(E)-2-(3-(3,4,5-trimethoxyphenyl)acryloyl)benzo[d]isothiazol-3(2H)-one
-
Homo sapiens
(E)-2-(3-(3,4,5-trimethoxyphenyl)acryloyl)isoindolin-1-one
-
Homo sapiens
(E)-3-((4-chlorophenyl)(hydroxy)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-((4-fluorophenyl)(hydroxy)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-(3-(3,4,5-trimethoxyphenyl)acryloyl)benzo[d]oxazol-2(3H)-one
-
Homo sapiens
(E)-3-(hydroxy(2-nitrophenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-(hydroxy(4-nitrophenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-(hydroxy(naphthalen-2-yl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-(hydroxy(p-tolyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-(hydroxy(phenyl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-(hydroxy(pyridin-2-yl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-3-(hydroxy(thiophen-2-yl)methyl)-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
(E)-4-(hydroxy(2-oxo-1-(3-(3,4,5-trimethoxyphenyl)acryloyl)-1,2,5,6-tetrahydropyridin-3-yl)methyl)benzonitrile
-
Homo sapiens
(E)-methyl 3-(3,4,5-trimethoxyphenyl)acrylate
-
Homo sapiens
(E)-N-ethanethioyl-3-(3,4,5-trimethoxyphenyl)acrylamide
-
Homo sapiens
1-((2E,4E)-5-(benzo[d][1,3]dioxol-5-yl)penta-2,4-dienoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-((2E,4E,6E)-7-(3,4,5-trimethoxyphenyl)hepta-2,4,6-trienoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(2-chlorobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(2-iodobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(1-benzyl-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(1-benzyl-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(1-benzyl-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(3,4,5-trimethoxyphenyl)-3-(1-methyl-1H-indol-3-yl)propanoyl)-4-(1-methyl-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(3,4,5-trimethoxyphenyl)-3-(1-methyl-1H-indol-3-yl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(3,4,5-trimethoxyphenyl)-3-(2-methyl-1H-indol-3-yl)propanoyl)-4-(2-methyl-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(3,4,5-trimethoxyphenyl)-3-(2-phenyl-1H-indol-3-yl)propanoyl)-4-(2-phenyl-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(3,4,5-trimethoxyphenyl)-3-(5-methoxy-1H-indol-3-yl)propanoyl)-4-(5-methoxy-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(3,4,5-trimethoxyphenyl)-3-(5-nitro-1H-indol-3-yl)propanoyl)-4-(5-nitro-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(3,4,5-trimethoxyphenyl)-3-(5-nitro-1H-indol-3-yl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(5-bromo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(5-bromo-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(5-bromo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(5-fluoro-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(5-fluoro-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(5-fluoro-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(5-iodo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-4-(5-iodo-1H-indol-3-yl)piperidin-2-one
-
Homo sapiens
1-(3-(5-iodo-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(3-(5-methoxy-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(4-fluorobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-(4-nitrobenzoyl)-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-cinnamoyl-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
1-[3-(2-phenyl-1H-indol-3-yl)-3-(3,4,5-trimethoxyphenyl)propanoyl]-5,6-dihydropyridin-2(1H)-one
-
Homo sapiens
3-(3,4,5-trimethoxyphenyl)-3-(2-methyl-1H-indol-3-yl)propanoic acid
-
Homo sapiens
5,6-dihydro-1-((E)-3-(3,4,5-trimethoxyphenyl)acryloyl)pyridin-2(1H)-one
-
Homo sapiens
fidarestat
-
Homo sapiens
imirestat
-
Homo sapiens
minalrestat
-
Homo sapiens
additional information inhibitor molecular docking study with ALR2, overview Homo sapiens
N-(2-phenylethyl)-N-{[4-(trifluoromethyl)phenyl]sulfonyl}glycine
-
Homo sapiens
piplartine
-
Homo sapiens
quercetin
-
Homo sapiens
sorbinil
-
Homo sapiens
Tolrestat
-
Homo sapiens
zopolrestat
-
Homo sapiens

Organism

Organism UniProt Comment Textmining
Homo sapiens
-
-
-

Source Tissue

Source Tissue Comment Organism Textmining
erythrocyte
-
Homo sapiens
-
kidney
-
Homo sapiens
-

Synonyms

Synonyms Comment Organism
aldose reductase
-
Homo sapiens
ALR2
-
Homo sapiens

Temperature Optimum [°C]

Temperature Optimum [°C] Temperature Optimum Maximum [°C] Comment Organism
37
-
assay at Homo sapiens

pH Optimum

pH Optimum Minimum pH Optimum Maximum Comment Organism
7.4
-
assay at Homo sapiens

IC50 Value

IC50 Value IC50 Value Maximum Comment Organism Inhibitor Structure
0.16
-
pH 7.4, 37°C Homo sapiens piplartine