Page last updated: 2024-09-27

sorbinil

Description

sorbinil: aldose reductase inhibitor [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

sorbinil : An azaspiro compound having a monofluoro-substituted chromane skeleton spiro-linked to an imidazolidinedione ring. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Cross-References

ID SourceID
PubMed CID337359
CHEMBL ID266497
CHEBI ID102029
SCHEMBL ID48877
MeSH IDM0086766

Synonyms (65)

Synonym
cp-45634
(4s)-6-fluoro-2,3-dihydro-2'h,5'h-spiro[chromene-4,4'-imidazolidine]-2',5'-dione
nsc355082
sorbinil
nsc-355082
mls003171137 ,
D05893
sorbinil (usan/inn)
68367-52-2
SBI ,
(4s)-6-fluoro-2,3-dihydrospiro[1-benzopyran-4,4''-imidazolidine]-2'',5''-dione
NCGC00159452-02
bdbm16312
DB02712
chembl266497 ,
sorbinilum
CHEBI:102029 ,
sorbinilo
(s)-6-fluorospiro(chroman-4,4'-imidazolidine)-2',5'-dione
AKOS000280386
(4s)-6-fluorospiro[2,3-dihydrochromene-4,5'-imidazolidine]-2',4'-dione
cp-45,634
cp 45634
HMS3260F11
g4186b906p ,
unii-g4186b906p
cp 45,634
spiro(4h-1-benzopyran-4,4'-imidazolidine)-2',5'-dione, 6-fluoro-2,3-dihydro-, (s)-
nsc 355082
sorbinilum [latin]
sorbinilo [spanish]
sorbinil [usan:inn:ban]
tox21_111679
dtxsid0023587 ,
cas-68367-52-2
dtxcid503587
sorbinil [inn]
sorbinil [usan]
sorbinil [who-dd]
sorbinil [mi]
sorbinil [mart.]
gtpl7415
(4s)-6-fluorospiro[chroman-4,5'-imidazolidine]-2',4'-dione
CCG-221489
SCHEMBL48877
tox21_111679_1
NCGC00159452-03
NCGC00260870-01
tox21_500185
cp45634
(s)(+)-6-fluoro-spiro-[chroman-4,4'-imidazolidine]-2',5'-dione
LXANPKRCLVQAOG-NSHDSACASA-N
(+)-(4s)-6-fluorospiro[chroman-4,4'-imidazolidine]-2',5'-dione
.beta.-l-gulopyranose, 1,6-anhydro-2,3-o-(phenylmethylene)-, (s)-
sorbinil, >=98% (hplc)
spiro[4h-1-benzopyran-4,4'-imidazolidine]-2',5'-dione,6-fluoro-2,3-dihydro-,(4s)-
HY-50289
(s)-6-fluorospiro[chromane-4,4'-imidazolidine]-2',5'-dione
112420-09-4
Q1259458
NCGC00159452-05
CS-0002274
MS-23366
(4s)-6-fluoro-2,3-dihydrospiro[1-benzopyran-4,4'-imidazolidine]-2',5'-dione
STARBLD0009657

Research Excerpts

Overview

ExcerptReference
"Sorbinil is an effective ARI, which could play therapeutic role in treating diabetes and diabetic complications. "( Huang, Q; Liu, Q; Ouyang, D, 2019)
"Sorbinil is a hydantoin aldose reductase inhibitor that has shown promise as therapy for patients with diabetic complications such as neuropathy and retinopathy. "( Cannon, M; Gunderson, K; Hutson, NJ; Shear, NH; Spielberg, SP, 1991)
"Sorbinil is a potent inhibitor of aldose reductase (the first enzyme in the polyol pathway) and has been shown to normalize sorbitol levels in relevant tissues (eg, nerve, kidney, lens) of experimentally-induced diabetic animals."( Aldinger, CE; Just, LJ; Malone, JI; Page, MG; Peterson, MJ, 1986)

Effects

ExcerptReference
"Sorbinil has no significant effect on the above metabolites in the normal rat lens."( Gonzalez, AM; McLean, P; Sochor, M, 1983)

Treatment

ExcerptReference
"Sorbinil treatment also induced functional recovery in myocardial fractional shortening in vivo and preserved contractile function of isolated perfused hearts."( Bhatnagar, A; DiMaio, JM; Horton, JW; Ramana, KV; Srivastava, D; Srivastava, SK; White, MD; Willis, MS, 2006)
"Sorbinil treatment (40 mg/kg) decreased the lens content of sorbitol to 0.60 +/- 0.06, fructose to 0.85 +/- 0.08, and glycerol 3-phosphate to 0.36 +/- 0.03 mumol/g; glucose 6-phosphate remained unchanged."( Gonzalez, AM; McLean, P; Sochor, M, 1983)
"Sorbinil treatment at 20 mg ."( Gillon, KR; Hawthorne, JN; Tomlinson, DR, 1983)
"Sorbinil treatment reduced the elevated sorbitol levels in the diabetic patients to normal or slightly below normal, but did not affect the erythrocyte myo-inositol concentration."( Lomecky-Janousek, MZ; Popp-Snijders, C; Schouten, JA; van der Veen, EA, 1984)
"Sorbinil treatment for 4 wk reduced sciatic nerve sorbitol concentration and improved motor nerve conduction velocity in diabetes of 2-9 mo duration."( Hanwell, MA; Satchell, PM; Turtle, JR; Yue, DK, 1982)
"Sorbinil treatment was associated with normalized sciatic nerve sorbitol and myo-inositol; ALC treatment did not reduce the elevated sorbitol levels, but sciatic nerve myo-inositol content was no different from nondiabetic levels."( Benford, S; Korthals, J; Lowitt, S; Malone, JI; Salem, AF, 1995)
"Ten sorbinil-treated patients showed significant improvement in axo-glial dysjunction, a characteristic lesion of the node of Ranvier."( Bril, V; Greene, DA; Nathaniel, V; Prashar, A; Sima, AA; Werb, MR, 1993)
"Sorbinil treatment did, however, alter responses of control left and right atria in a manner similar to diabetes."( Chess-Williams, R; Sellers, DJ, 2000)
"Sorbinil treatment essentially corrected diabetes-induced sorbitol and fructose accumulation, myo-inositol depletion, decrease in free cytosolic NAD+:NADH ratio and energy deficiency."( Fathallah, L; Obrosova, IG, 2000)
"4. Sorbinil treatment of diabetic animals failed to prevent any of these diabetes-induced alterations in aortic function, and indeed exacerbated some of these alterations."( Chess-Williams, R; Sellers, DJ, 2000)
"Sorbinil treatment completely prevented renal cortical sorbital accumulation, but did not abolish kidney enlargement or the increase in ultrafiltration pressure and glomerular filtration rate."( Aperia, A; Celsi, G; Eklöf, AC; Körner, A; Linné, T; Persson, B, 1992)
"Sorbinil treatment was continued throughout the hyper- and hyponatremic periods."( Futterweit, S; Hammer, E; Oates, P; Siegel, TW; Trachtman, H, 1991)
"Sorbinil treatment markedly reduced or completely prevented all of these changes in galactose-fed, as well as in diabetic rats."( Chang, K; Kilo, C; Province, MA; Pugliese, G; Speedy, A; Tilton, RG; Williamson, JR, 1990)
"Sorbinil treatment completely abolished the formation of this protein."( Monnier, VM; Nagaraj, RH, 1990)
"Sorbinil treatment of diabetic animals was associated with normalization of both lens sorbitol and taurine levels."( Cook, WR; Lowitt, S; Malone, JI, 1990)
"Sorbinil treatment prevented approximately 70% of the increase in total protein excretion despite persistent hyperglycemia, glycosuria and ketonuria."( Beyer-Mears, A; Cruz, E; Edelist, T; Varagiannis, E, 1986)
"Sorbinil treatment prevented the 10-fold increase in nerve sorbitol found with diabetes."( Cameron, NE; Leonard, MB; Ross, IS; Whiting, PH, 1986)
"Sorbinil treatment failed to improve even slightly the abnormalities in cellular replication induced by high glucose."( Boss, GR; Lane, MJ; Lorenzi, M; Montisano, DF; Toledo, S, 1987)
"Sorbinil treatment, initiated after 8 weeks of diabetes, and without effect on sciatic nerve glucose levels, normalized sorbitol concentrations following 4, 8, or 12 weeks of treatment but only partially reversed the accumulation of fructose by 368, 161 and 199%, compared to age-matched non-diabetic control values, at the above times, respectively."( Ross, IS; Whiting, PH, 1988)
"Treatment with sorbinil blunted the activation of protein kinase C, c-Jun NH2-terminal kinase, and p38, as well as phosphorylation of interleukin receptor-associated kinase, IkappaB-alpha, IkappaB kinase complex-alpha/beta, and phospholipase-gamma1 and -beta1."( Bhatnagar, A; DiMaio, JM; Horton, JW; Ramana, KV; Srivastava, D; Srivastava, SK; White, MD; Willis, MS, 2006)
"Treatment with Sorbinil (25 mg/kg/day, p.o.) throughout the period of diabetes prevented the development of all these abnormalities in both 3- and 6-wk diabetic groups."( Mayer, JH; Moriarty, RJ; Tomlinson, DR, 1984)
"ARI treatment with sorbinil failed to prevent all but one of these changes, and in addition altered responses of atria from control rats, having a similar effect to that produced by diabetes."( Chess-Williams, R; Sellers, DJ, 2000)
"Treatment with sorbinil was associated with normalization of the tissue sorbitol (0.10 +/- 0.05 nm/mg ww), while ALC treatment also significantly reduced the nerve sorbitol but only to a level (0.34 +/- 0.08 nm/mg ww) more elevated than the normal level."( Corsico, N; Lowitt, S; Malone, JI; Orfalian, Z, 1992)
"3. Treatment with sorbinil for 30 days after induction of diabetes did not influence the increased fluorescence observed in collagen from glomerular basement membrane of untreated diabetic rats."( Cohen, MP; Klepser, H; Wu, VY, 1991)

Roles (2)

RoleDescription
EC 1.1.1.21 (aldehyde reductase) inhibitorAn EC 1.1.1.* (oxidoreductase acting on donor CH-OH group, NAD(+) or NADP(+) acceptor) inhibitor that interferes with the action of aldehyde reductase (EC 1.1.1.21).
antioxidantA substance that opposes oxidation or inhibits reactions brought about by dioxygen or peroxides.
[role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Drug Classes (5)

ClassDescription
chromanes
oxaspiro compoundA spiro compound in which at least one of the cyclic components is an oxygen heterocyle.
azaspiro compoundAn azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle.
organofluorine compoundAn organofluorine compound is a compound containing at least one carbon-fluorine bond.
imidazolidinoneAn imidazolidine containing one or more oxo groups.
[compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]

Protein Targets (15)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency33.49150.006038.004119,952.5996AID1159521
Microtubule-associated protein tauHomo sapiens (human)Potency8.91250.180013.557439.8107AID1468
AR proteinHomo sapiens (human)Potency29.76290.000221.22318,912.5098AID743042; AID743054; AID743063
ATP-dependent phosphofructokinaseTrypanosoma brucei brucei TREU927Potency35.48130.060110.745337.9330AID492961
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Inhibition Measurements

ProteinTaxonomyMeasurementAverageMin (ref.)Avg (ref.)Max (ref.)Bioassay(s)
Aldo-keto reductase family 1 member B10Homo sapiens (human)IC50 (µMol)5.05000.00101.94459.6000AID1802103; AID489631
Aldo-keto reductase family 1 member B1Rattus norvegicus (Norway rat)IC50 (µMol)0.86980.00041.877310.0000AID1142509; AID1335654; AID1478797; AID1478798; AID1589443; AID241371; AID34795; AID34798; AID34799; AID34803; AID34804; AID34805; AID34814; AID34962; AID34964; AID34965; AID34969; AID34970; AID34973; AID34974; AID34975; AID381848; AID462440; AID95257
5-hydroxytryptamine receptor 1AHomo sapiens (human)IC50 (µMol)0.50000.00010.666410.0000AID34638
Aldo-keto reductase family 1 member A1Homo sapiens (human)IC50 (µMol)5.13330.00502.78569.9000AID242590; AID34177; AID489639
Aldo-keto reductase family 1 member B1Homo sapiens (human)IC50 (µMol)121.22890.00101.191310.0000AID1589441; AID159818; AID159820; AID1646335; AID1646336; AID1700253; AID1713572; AID1797505; AID1802103; AID220720; AID241413; AID255041; AID309933; AID322413; AID34201; AID34634; AID34637; AID34638; AID34641; AID34646; AID34648; AID34650; AID34653; AID34654; AID34655; AID34782; AID34783; AID462442; AID477037; AID489638
Alpha-1B adrenergic receptorRattus norvegicus (Norway rat)IC50 (µMol)3.04000.00021.874210.0000AID35134
Aldo-keto reductase family 1 member B1Bos taurus (cattle)IC50 (µMol)1.72920.00702.589210.0000AID1143289; AID299415; AID34210; AID34211; AID34505; AID34506; AID35132; AID35134; AID35135; AID35136; AID488380; AID549694
Aldo-keto reductase family 1 member A1Sus scrofa (pig)IC50 (µMol)2.95000.00051.66804.0000AID242609; AID34178
Aldo-keto reductase family 1 member A1Rattus norvegicus (Norway rat)IC50 (µMol)0.88450.02801.13782.3200AID34196; AID34198
Aldo-keto reductase family 1 member B1Sus scrofa (pig)IC50 (µMol)1.10000.01500.61352.5000AID241043
Mu-type opioid receptorCavia porcellus (domestic guinea pig)IC50 (µMol)1.10000.00020.660310.0000AID241043
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Biological Processes (37)

Processvia Protein(s)Taxonomy
retinoid metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
farnesol catabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member B10Homo sapiens (human)
cellular detoxification of aldehydeAldo-keto reductase family 1 member B10Homo sapiens (human)
behavioral fear response5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
adenylate cyclase-inhibiting serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin receptor signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
gamma-aminobutyric acid signaling pathway5-hydroxytryptamine receptor 1AHomo sapiens (human)
positive regulation of cell population proliferation5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of serotonin secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of vasoconstriction5-hydroxytryptamine receptor 1AHomo sapiens (human)
exploration behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of dopamine metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin metabolic process5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of hormone secretion5-hydroxytryptamine receptor 1AHomo sapiens (human)
regulation of behavior5-hydroxytryptamine receptor 1AHomo sapiens (human)
chemical synaptic transmission5-hydroxytryptamine receptor 1AHomo sapiens (human)
G protein-coupled receptor signaling pathway, coupled to cyclic nucleotide second messenger5-hydroxytryptamine receptor 1AHomo sapiens (human)
lipid metabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
glucuronate catabolic process to xylulose 5-phosphateAldo-keto reductase family 1 member A1Homo sapiens (human)
L-ascorbic acid biosynthetic processAldo-keto reductase family 1 member A1Homo sapiens (human)
D-glucuronate catabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
negative regulation of apoptotic processAldo-keto reductase family 1 member A1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
aldehyde catabolic processAldo-keto reductase family 1 member A1Homo sapiens (human)
cellular detoxification of aldehydeAldo-keto reductase family 1 member A1Homo sapiens (human)
glutathione derivative biosynthetic processAldo-keto reductase family 1 member A1Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
epithelial cell maturationAldo-keto reductase family 1 member B1Homo sapiens (human)
renal water homeostasisAldo-keto reductase family 1 member B1Homo sapiens (human)
carbohydrate metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
C21-steroid hormone biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
L-ascorbic acid biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
regulation of urine volumeAldo-keto reductase family 1 member B1Homo sapiens (human)
retinol metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
negative regulation of apoptotic processAldo-keto reductase family 1 member B1Homo sapiens (human)
daunorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
doxorubicin metabolic processAldo-keto reductase family 1 member B1Homo sapiens (human)
fructose biosynthetic processAldo-keto reductase family 1 member B1Homo sapiens (human)
cellular hyperosmotic salinity responseAldo-keto reductase family 1 member B1Homo sapiens (human)
metanephric collecting duct developmentAldo-keto reductase family 1 member B1Homo sapiens (human)
retinoid metabolic processAldo-keto reductase family 1 member B1Bos taurus (cattle)
prostaglandin metabolic processAldo-keto reductase family 1 member B1Bos taurus (cattle)
retinol metabolic processAldo-keto reductase family 1 member B1Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Molecular Functions (23)

Processvia Protein(s)Taxonomy
retinal dehydrogenase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member B10Homo sapiens (human)
alcohol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
geranylgeranyl reductase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
indanol dehydrogenase activityAldo-keto reductase family 1 member B10Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member B10Homo sapiens (human)
G protein-coupled serotonin receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
protein binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
receptor-receptor interaction5-hydroxytryptamine receptor 1AHomo sapiens (human)
neurotransmitter receptor activity5-hydroxytryptamine receptor 1AHomo sapiens (human)
serotonin binding5-hydroxytryptamine receptor 1AHomo sapiens (human)
all-trans-retinol dehydrogenase (NAD+) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
aldo-keto reductase (NADPH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member A1Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member A1Homo sapiens (human)
L-glucuronate reductase activityAldo-keto reductase family 1 member A1Homo sapiens (human)
glucuronolactone reductase activityAldo-keto reductase family 1 member A1Homo sapiens (human)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member A1Homo sapiens (human)
S-nitrosoglutathione reductase (NADH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
S-nitrosoglutathione reductase (NADPH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
methylglyoxal reductase (NADPH) (acetol producing) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member A1Homo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
aldose reductase (NADPH) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
protein bindingAldo-keto reductase family 1 member B1Homo sapiens (human)
electron transfer activityAldo-keto reductase family 1 member B1Homo sapiens (human)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glyceraldehyde oxidoreductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
L-glucuronate reductase activityAldo-keto reductase family 1 member B1Homo sapiens (human)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member B1Homo sapiens (human)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B1Homo sapiens (human)
retinal dehydrogenase activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
prostaglandin H2 endoperoxidase reductase activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
allyl-alcohol dehydrogenase activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
glycerol dehydrogenase [NADP+] activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
all-trans-retinol dehydrogenase (NADP+) activityAldo-keto reductase family 1 member B1Bos taurus (cattle)
[Information is prepared from geneontology information from the June-17-2024 release]

Ceullar Components (11)

Processvia Protein(s)Taxonomy
extracellular regionAldo-keto reductase family 1 member B10Homo sapiens (human)
lysosomeAldo-keto reductase family 1 member B10Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B10Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B10Homo sapiens (human)
mitochondrionAldo-keto reductase family 1 member B10Homo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
synapse5-hydroxytryptamine receptor 1AHomo sapiens (human)
plasma membrane5-hydroxytryptamine receptor 1AHomo sapiens (human)
dendrite5-hydroxytryptamine receptor 1AHomo sapiens (human)
extracellular spaceAldo-keto reductase family 1 member A1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member A1Homo sapiens (human)
synapseAldo-keto reductase family 1 member A1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member A1Homo sapiens (human)
apical plasma membraneAldo-keto reductase family 1 member A1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member A1Homo sapiens (human)
extracellular spaceAldo-keto reductase family 1 member B1Homo sapiens (human)
nucleoplasmAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
extracellular exosomeAldo-keto reductase family 1 member B1Homo sapiens (human)
cytosolAldo-keto reductase family 1 member B1Homo sapiens (human)
[Information is prepared from geneontology information from the June-17-2024 release]

Bioassays (212)

Assay IDTitleYearJournalArticle
AID182013Compound was evaluated in vivo for the inhibition of sorbitol accumulation administered orally at a dose of 0.25 mg/kg.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners.
AID34506Inhibitory activity against bovine lens aldose reductase1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil.
AID34804In vitro inhibitory activity against aldose reductase (ALR2) from rat lens extraction.2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.
AID489641Selectivity ratio of IC50 for human ALR to IC50 for AKR1B102010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
AID1589440Inhibition of human recombinant ALR2 expressed in Escherichia coli using DL-glyceraldehyde as substrate and NADPH at 50 uM preincubated for 5 mins followed by substrate addition and measured after 30 mins at 2 mins interval by spectrophotometry relative t2019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID34788In vitro inhibition of rabbit lens aldose reductase at 10e-5 M.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
AID34799Compound was tested for its ability to inhibit crude aldose reductase obtained from rat lens1986Journal of medicinal chemistry, May, Volume: 29, Issue:5
Design and synthesis of 2-(arylamino)-4(3H)-quinazolinones as novel inhibitors of rat lens aldose reductase.
AID34653Inhibitory activity against human placental aldose reductase in Sepharose 4B column at day 71985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID184947Tested in vivo for ability to inhibit sorbitol formation in the lens of a streptozotocinized rat model after oral administration at the dose of 0.15 mg/Kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID34970Inhibitory concentration against aldose reductase obtained from rat lens1989Journal of medicinal chemistry, Jan, Volume: 32, Issue:1
N- and 2-substituted N-(phenylsulfonyl)glycines as inhibitors of rat lens aldose reductase.
AID241413Inhibitory concentration against human ALR22005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID230202Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W111A)2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.
AID233810The ratio of the inhibitory concentration causing a 50% reduction of sorbitol in the isolated nerve to the IC50 in the isolated enzyme1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID232928Selectivity as ratio of IC50 for rat lens and kidney aldose reductase1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors.
AID220720In vitro inhibitory activity against human recombinant Aldose reductase in streptozotocin diabetic rat at 50 mg/kg2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
AID241371Inhibitory concentration against rat ALR2 aldose reductase2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID1315347In vivo inhibition of aldose reductase in wild type mouse assessed as reduction in vacuolization at 80 mg/kg, po for 16 days by hematoxylin/eosin staining2016Journal of natural products, 05-27, Volume: 79, Issue:5
Characterization of Emodin as a Therapeutic Agent for Diabetic Cataract.
AID1478797Inhibition of Sprague-Dawley rat lens ALR2 using D,L-glyceraldehyde as substrate preincubated for 10 mins followed by substrate addition measured for 5 mins by spectrophotometric method2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
N-(Aroyl)-N-(arylmethyloxy)-α-alanines: Selective inhibitors of aldose reductase.
AID381848Inhibition of aldose reductase in rat lenses2008Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7
Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors.
AID1589441Inhibition of human recombinant ALR2 expressed in Escherichia coli using DL-glyceraldehyde as substrate and NADPH preincubated for 5 mins followed by substrate addition and measured after 30 mins at 2 mins interval by spectrophotometry relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID1066260Inhibition of AKR1B1 in mouse RAW264.7 cells assessed as inhibition of sorbitol accumulation after 24 hrs by colorimetric assay2014Journal of medicinal chemistry, Jan-09, Volume: 57, Issue:1
Design of an amide N-glycoside derivative of β-glucogallin: a stable, potent, and specific inhibitor of aldose reductase.
AID177265Compound was evaluated for the ED50(chronic) in male Sprague-Dawley rats(n=4) treated with streptozotocin (85 mg/kg intravenously).1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners.
AID182014Compound was evaluated in vivo for the inhibition of sorbitol accumulation administered orally at a dose of 0.75 mg/kg.1991Journal of medicinal chemistry, Jan, Volume: 34, Issue:1
Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners.
AID322411Inhibition of mouse recombinant AKR1C21 at 50 uM2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.
AID1315351In vivo inhibition of aldose reductase in transgenic PAR37 mouse expressing human aldose reductase assessed as vacuolization at 80 mg/kg, po for 16 days by hematoxylin/eosin staining (Rvb = 18%)2016Journal of natural products, 05-27, Volume: 79, Issue:5
Characterization of Emodin as a Therapeutic Agent for Diabetic Cataract.
AID203729Inhibition of sorbitol dehydrogenase from sheep liver (40 U/mg of protein)1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis, activity, and molecular modeling of a new series of tricyclic pyridazinones as selective aldose reductase inhibitors.
AID34354In vitro aldose reductase inhibitory activity measured by NADPH-dependent inhibition of glyceraldehyde reduction in a partially purified bovine lens preparation at 10E-6 M1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Novel spirosuccinimides with incorporated isoindolone and benzisothiazole 1,1-dioxide moieties as aldose reductase inhibitors and antihyperglycemic agents.
AID184331In vivo galactitol inhibitory activity measured by its ability to inhibit galactitol accumulation in diaphragm at 4 mg/Kg/day1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Novel spirosuccinimides with incorporated isoindolone and benzisothiazole 1,1-dioxide moieties as aldose reductase inhibitors and antihyperglycemic agents.
AID75435Evaluated for inhibition of glutathione reductase.; No inhibition1996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis, activity, and molecular modeling of a new series of tricyclic pyridazinones as selective aldose reductase inhibitors.
AID379162Inhibition of human recombinant ALR22006Journal of natural products, Oct, Volume: 69, Issue:10
Phenolic marine natural products as aldose reductase inhibitors.
AID182432In vivo inhibition of galactitol accumulation in the sciatic nerves of rat at a dose of 4 mg/kg/day1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat.
AID184961Tested in vivo for ability to inhibit sorbitol formation in the nerve of a streptozotocinized rat model after oral administration at the dose of 0.75 mg/kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID34798Compound was tested for inhibitory concentration against rat lens aldose reductase (uncompetitive inhibition type)1986Journal of medicinal chemistry, Jun, Volume: 29, Issue:6
Synthesis and rat lens aldose reductase inhibitory activity of some benzopyran-2-ones.
AID309933Inhibition of aldose reductase2007Bioorganic & medicinal chemistry, Dec-15, Volume: 15, Issue:24
Validation of an automated procedure for the prediction of relative free energies of binding on a set of aldose reductase inhibitors.
AID34964Inhibitory activity measured against rat lens aldose reductase using 3-pyridinecarboxaldehyde as substrate1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
AID468476Inhibition of Albino rat eye lens ALR2 assessed as NADPH oxidation by spectrophotometry2010European journal of medicinal chemistry, Mar, Volume: 45, Issue:3
Synthesis and biological evaluation of [1,2,4]triazino[4,3-a] benzimidazole acetic acid derivatives as selective aldose reductase inhibitors.
AID34637In vitro inhibitory activity against recombinant human aldose reductase (ALR2) was determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Synthesis, activity, and molecular modeling studies of novel human aldose reductase inhibitors based on a marine natural product.
AID549694Inhibition of bovine lens aldose reductase assessed as inhibition of NDAPH oxidation by non-linear regression analysis2011Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1
In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors.
AID35109In vitro inhibitory activity against aldose reductase of rat lens at 2.5x10E-7 M concentration2003Journal of medicinal chemistry, Jan-30, Volume: 46, Issue:3
Substituted pyrrol-1-ylacetic acids that combine aldose reductase enzyme inhibitory activity and ability to prevent the nonenzymatic irreversible modification of proteins from monosaccharides.
AID537153Inhibition of rat lens ALR22010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
AID489639Inhibition of N-terminal 6His-tagged human aldehyde reductase expressed in Escherichia coli BL21(DE3) mediated D-glucuronate reduction2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
AID34355In vitro aldose reductase inhibitory activity measured by NADPH-dependent inhibition of glyceraldehyde reduction in a partially purified bovine lens preparation at 10E-7 M1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Novel spirosuccinimides with incorporated isoindolone and benzisothiazole 1,1-dioxide moieties as aldose reductase inhibitors and antihyperglycemic agents.
AID34654Inhibitory activity against human placental aldose reductase in Sepharose 4B column at time 11985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID1700253Inhibition of ALR2 (unknown origin)2020Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24
Synthesis and biological screening of thiosemicarbazones of substituted 3-acetylcoumarins having d-glucose moiety.
AID177556Ability to cause 50% reduction in sorbitol levels of sciatic nerve of streptozotocinized rats was determined1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID34965Inhibitory activity against aldose reductase in rat lens1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Relative structure-inhibition analyses of the N-benzoyl and N-(phenylsulfonyl) amino acid aldose reductase inhibitors.
AID34655Tested for in vitro inhibition activity against human Aldose reductase (human AR)2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.
AID1589444Selectivity ratio of IC50 for rat kidney ALR1 IC50 to IC50 for human recombinant ALR22019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID35113In vitro percentage inhibition of rat lens aldose reductase at 10E-6 M concentration2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
[1-(3,5-difluoro-4-hydroxyphenyl)-1H-pyrrol-3-yl]phenylmethanone as a bioisostere of a carboxylic acid aldose reductase inhibitor.
AID184964Tested in vivo for ability to inhibit sorbitol formation in the nerve of a streptozotocinized rat model after oral administration at the dose of 2.5 mg/Kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID322413Inhibition of human recombinant aldose reductase2008Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6
Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors.
AID35133Compound was tested for Ratio of IC50(ALR1)/(ALR2)1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
AID462440Inhibition of aldose reductase in Fischer-344 rat lens homogenate by spectrometric analysis2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.
AID178946Effective dose required to inhibit sorbitol accumulation in sciatic nerves of streptozotocinized rats administered perorally1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil.
AID34641Inhibitory activity against human placenta aldose reductase1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil.
AID34786In vitro inhibition of rabbit lens aldose reductase at 10e-4 M.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
AID75439In vitro inhibitory activity against glutathione reductase (GR) from bakers yeast; Not active2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.
AID34475Inhibition of aldose reductase in partially purified bovine lens preparation at 10e-6 M.1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat.
AID184953Tested in vivo for ability to inhibit sorbitol formation in the lens of a streptozotocinized rat model after oral administration at the dose of 1.5 mg/Kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID26108pKa value for the compound was determined1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Isoxazolidine-3,5-diones as lens aldose reductase inhibitors.
AID159818Inhibition of human placental aldose reductase (HPAR) activity with glyceraldehyde as substrate1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors.
AID1124833Inhibition of Fischer-344 rat lens ALR2 using D, L-glyceraldehyde as substrate by spectrophotometry2014Bioorganic & medicinal chemistry, Apr-01, Volume: 22, Issue:7
Decreasing acidity in a series of aldose reductase inhibitors: 2-Fluoro-4-(1H-pyrrol-1-yl)phenol as a scaffold for improved membrane permeation.
AID184954Tested in vivo for ability to inhibit sorbitol formation in the lens of a streptozotocinized rat model after oral administration at the dose of 2.5 mg/Kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID34505Inhibition of bovine lens aldose reductase with DL-glyceraldehyde as substrate1984Journal of medicinal chemistry, Mar, Volume: 27, Issue:3
N-[5-(trifluoromethyl)-6-methoxy-1-naphthalenyl]thioxomethyl]- N-methylglycine (Tolrestat), a potent, orally active aldose reductase inhibitor.
AID35135In vitro inhibitory activity against Aldose reductase 2 obtained from calf lenses1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
Isoxazolo-[3,4-d]-pyridazin-7-(6H)-one as a potential substrate for new aldose reductase inhibitors.
AID34634In vitro inhibitory activity against Aldose reductase isolated from human placenta1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID254230Binding constant against wild-type human aldose reductase at 18.9 uM2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.
AID1589442Inhibition of rat kidney ALR1 using DL-glyceraldehyde as substrate and NADPH at 50 uM preincubated for 5 mins followed by substrate addition and measured for 30 mins at 2 mins interval by spectrophotometry relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID34650Inhibitory activity against human placental aldose reductase in Orange A column at day 81985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID34646Inhibitory activity against human placental aldose reductase in 30 -70% (NH4)2SO4.1985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID230203Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W111Y).2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.
AID34969Inhibitory concentration to aldose reductase (ALR-2) obtained from rat lens2001Journal of medicinal chemistry, Dec-06, Volume: 44, Issue:25
[1,2,4]Triazino[4,3-a]benzimidazole acetic acid derivatives: a new class of selective aldose reductase inhibitors.
AID179749In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-6 M concentration1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID462442Inhibition of aldose reductase2010Bioorganic & medicinal chemistry, Mar-15, Volume: 18, Issue:6
Design and synthesis of novel series of pyrrole based chemotypes and their evaluation as selective aldose reductase inhibitors. A case of bioisosterism between a carboxylic acid moiety and that of a tetrazole.
AID182579In vivo inhibition of sorbitol accumulation in rat sciatic nerves at 10e-5 M concentration1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat.
AID194291Compound was evaluated in vivo for percent inhibition of polyol accumulation at a dose of 3 mg/kg per day.1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors.
AID477037Inhibition of aldose reductase2010European journal of medicinal chemistry, Apr, Volume: 45, Issue:4
Evaluation of aldose reductase inhibition and docking studies of 6'-nitro and 6',6''-dinitrorosmarinic acids.
AID34975In vitro inhibition of Aldose reductase (AR) from rat lens (RL)1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors.
AID1443999Inhibition of Fischer-344 rat lens ALR22017European journal of medicinal chemistry, Apr-21, Volume: 130Enhancing activity and selectivity in a series of pyrrol-1-yl-1-hydroxypyrazole-based aldose reductase inhibitors: The case of trifluoroacetylation.
AID1315345In vivo inhibition of aldose reductase in transgenic PAR37 mouse expressing human aldose reductase assessed as reduction in vacuolization at 80 mg/kg, po for 16 days by hematoxylin/eosin staining2016Journal of natural products, 05-27, Volume: 79, Issue:5
Characterization of Emodin as a Therapeutic Agent for Diabetic Cataract.
AID107292Compound was evaluated for its analgesic activity in mice by mouse phenylquinone writhing assay, and the activity relative to aspirin was reported; Not tested1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
AID603256Inhibition of bovine lens ALR22011European journal of medicinal chemistry, Jul, Volume: 46, Issue:7
Identification of 5-arylidene-4-thiazolidinone derivatives endowed with dual activity as aldose reductase inhibitors and antioxidant agents for the treatment of diabetic complications.
AID203732In vitro inhibitory activity against sorbitol dehydrogenase (SD) from sheep liver; Not active2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.
AID182593In vivo inhibition of sorbitol accumulation in rat sciatic nerves at 5*10e-6 M concentration1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat.
AID489631Inhibition of reductase activity of N-terminal 6His-tagged AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as inhibition of NADPH linked pyridine-3-aldehyde reduction2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
AID34783Tested in vitro for inhibitory activity against partially purified aldose reductase from male rabbit lens1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors.
AID35136Inhibition of Aldose reductase 2 of bovine lens1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
AID34177Tested for in vitro inhibition activity against human aldehyde reductase (AHR)2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.
AID230204Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W20A).2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.
AID34351In vitro % decrease of aldose reductase measured in isolated partially purified bovine lens preparations at 10e-7 M concentration1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID1646335Inhibition of human recombinant AKR1B1 assessed as D,L-glyceraldehyde reduction pretreated with 0.3M DMSO followed by compound addition by DMSO-perturbation assay2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Early identification of promiscuous attributes of aldose reductase inhibitors using a DMSO-perturbation assay.
AID34638In vitro inhibitory activity towards human placenta aldose reductase1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID34795Inhibition of crude aldose reductase of rat lens1986Journal of medicinal chemistry, Oct, Volume: 29, Issue:10
Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives.
AID537152Inhibition of Fischer-344 rat lens ALR2 at 0.25 uM2010Journal of medicinal chemistry, Nov-11, Volume: 53, Issue:21
A diverse series of substituted benzenesulfonamides as aldose reductase inhibitors with antioxidant activity: design, synthesis, and in vitro activity.
AID299415Inhibition of bovine aldose reductase2007Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14
Evaluation of in vitro aldose redutase inhibitory activity of 5-arylidene-2,4-thiazolidinediones.
AID18149650% reduction in sorbitol accumulation in isolated sciatic nerves incubated in the presence of high glucose concentration1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID34789In vitro inhibition of rabbit lens aldose reductase at 10e-6 M.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
AID184958Tested in vivo for ability to inhibit sorbitol formation in the nerve of a streptozotocinized rat model after oral administration at the dose of 0.15 mg/Kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID241043Inhibition of aldose reductase from pig lenses2004Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21
Soft docking and multiple receptor conformations in virtual screening.
AID232953Inhibitory activity measured against pig kidney aldehyde reductase using 3-pyridinecarboxaldehyde as substrate1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
AID184354In vivo galactitol inhibitory activity measured by its ability to inhibit galactitol accumulation in lens at 4 mg/Kg/day1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Novel spirosuccinimides with incorporated isoindolone and benzisothiazole 1,1-dioxide moieties as aldose reductase inhibitors and antihyperglycemic agents.
AID29166Dissociation constant was determined2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
AID184963Tested in vivo for ability to inhibit sorbitol formation in the nerve of a streptozotocinized rat model after oral administration at the dose of 1.5 mg/Kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID34664Selectivity ratio measured as the IC50 ratio of aldehyde/aldose reductase values1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
AID34210In vitro % decrease of aldose reductase was measured in isolated partially purified bovine lens preparations at 10e-6 M concentration1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID35115Inhibition of rat lens aldose reductase at 50 uM1982Journal of medicinal chemistry, Jun, Volume: 25, Issue:6
Isoxazolidine-3,5-diones as lens aldose reductase inhibitors.
AID408834Inhibition of bovine lens ALR2 assessed as reduction of D,L-glyceraldehyde by spectrophotometry2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives.
AID34198In vitro inhibitory activity against aldehyde reductase 1 (ALR1) from rat kidney.2003Journal of medicinal chemistry, Apr-10, Volume: 46, Issue:8
Novel, highly potent aldose reductase inhibitors: cyano(2-oxo-2,3-dihydroindol-3-yl)acetic acid derivatives.
AID176729Dose causing 50% reduction in sorbitol accumulation in isolated sciatic nerves of streptozotocinized rats, (tid)1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID256543Binding constant against Leu300Pro mutant of aldose reductase at 37.8 uM2005Journal of medicinal chemistry, Sep-08, Volume: 48, Issue:18
Factorizing selectivity determinants of inhibitor binding toward aldose and aldehyde reductases: structural and thermodynamic properties of the aldose reductase mutant Leu300Pro-fidarestat complex.
AID34648Inhibitory activity against human placental aldose reductase in Orange A column at at time 21985Journal of medicinal chemistry, Jul, Volume: 28, Issue:7
Aldose reductase inhibitors: a potential new class of agents for the pharmacological control of certain diabetic complications.
AID35134Evaluated for inhibition of Aldose reductase 21996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis, activity, and molecular modeling of a new series of tricyclic pyridazinones as selective aldose reductase inhibitors.
AID182251In vivo inhibition of galactitol accumulation in sciatic nerves of rat at 4 mg/kg/day1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID34985Compound was tested for percent inhibition of aldose reductase inhibitory activity using rat lens assay at concentration of 100 uM; ND= not determined1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Novel inhibitors of rat lens aldose reductase: N-[[(substituted amino)phenyl]sulfonyl]glycines.
AID34661Inhibitory activity measured against human placental aldose reductase at a concentration of 10e-5 M1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
AID34962Inhibitory activity against rat lens aldose reductase1985Journal of medicinal chemistry, Nov, Volume: 28, Issue:11
Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil.
AID1713572Inhibition of recombinant human ALR2 using D,L-glyceraldehyde and NADPH as substrate preincubated for 3 mins followed by substrate addition and measured for 3 mins by spectrophotometric analysis2016Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20
Pterin-7-carboxamides as a new class of aldose reductase inhibitors.
AID93598Inhibitory activity on sorbital accumulation in human retinal cells was determined2003Journal of medicinal chemistry, Nov-20, Volume: 46, Issue:24
Synthesis, activity, and molecular modeling studies of novel human aldose reductase inhibitors based on a marine natural product.
AID488380Inhibition of bovine lens aldose reductase2010Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11
Identification of new non-carboxylic acid containing inhibitors of aldose reductase.
AID170935Compound was evaluated in vivo for 50% inhibition of enzymatic activity of partially purified AR from male rabbit lens at a dose of 15 mg/kg per day; Polyol contents1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors.
AID242609Inhibitory concentration against porcine ALR1 Aldehyde reductase using DL-glyceraldehyde2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID34196Evaluated for inhibition of Aldehyde reductase 11996Journal of medicinal chemistry, Oct-25, Volume: 39, Issue:22
Synthesis, activity, and molecular modeling of a new series of tricyclic pyridazinones as selective aldose reductase inhibitors.
AID34782In vitro inhibition of rabbit lens aldose reductase.1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
AID182073In vivo inhibition of galactitol accumulation in diaphragm of rat at 4 mg/kg/day1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID182408In vivo inhibition of galactitol accumulation in the diaphragm of rat at a dose of 4 mg/kg/day1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat.
AID35127Inhibition of partially purified aldose reductase obtained from rat lens (100 uM ); ND is No Data1989Journal of medicinal chemistry, May, Volume: 32, Issue:5
Synthesis and in vitro aldose reductase inhibitory activity of compounds containing an N-acylglycine moiety.
AID182586In vivo inhibition of sorbitol accumulation in rat sciatic nerves at 10e-6 M concentration1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat.
AID34178Inhibitory activity measured against pig kidney aldehyde reductase using 3-pyridinecarboxaldehyde as substrate1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
AID720961Inhibition of Fischer-344 rat lens ALR2 using D-glycuronate as substrate by spectrophotometry2013Bioorganic & medicinal chemistry, Feb-15, Volume: 21, Issue:4
Synthesis of derivatives of the keto-pyrrolyl-difluorophenol scaffold: some structural aspects for aldose reductase inhibitory activity and selectivity.
AID1646336Inhibition of human recombinant AKR1B1 assessed as D,L-glyceraldehyde reduction pretreated with 0.7M DMSO followed by compound addition by DMSO-perturbation assay2020Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2
Early identification of promiscuous attributes of aldose reductase inhibitors using a DMSO-perturbation assay.
AID194289Compound was evaluated in vivo for percent inhibition of polyol accumulation at a dose of 15 mg/kg per day1992Journal of medicinal chemistry, May-29, Volume: 35, Issue:11
Biological activities and quantitative structure-activity relationships of spiro[imidazolidine-4,4'(1'H)-quinazoline]-2,2',5(3'H)-triones as aldose reductase inhibitors.
AID178209Effective dose of aldose reductase was evaluated by measuring galactitol accumulation in sciatic nerves of rat at 4 mg/kg/day1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID34973Tested for in vitro inhibition activity against rat Aldose reductase (AR)2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.
AID34662Inhibitory activity measured against human placental aldose reductase at a concentration of 10e-6 M1991Journal of medicinal chemistry, Mar, Volume: 34, Issue:3
A highly specific aldose reductase inhibitor, ethyl 1-benzyl-3-hydroxy-2(5H)-oxopyrrole-4-carboxylate, and its congeners.
AID34211In vitro % decrease of aldose reductase was measured in isolated partially purified bovine lens preparations at 10e-7 M concentration1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID95257In vitro inhibitory activity against L-Hexonate Dehydrogenase (L-HDH) from rat kidney (RK)1991Journal of medicinal chemistry, Nov, Volume: 34, Issue:11
Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors.
AID489640Selectivity ratio of IC50 for human AR to IC50 for AKR1B102010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
AID1142509Inhibition of aldose reductase in rat lens by spectrophotometer analysis2014European journal of medicinal chemistry, Jun-10, Volume: 80Synthesis and biological evaluation of some new pyrazoline substituted benzenesulfonylurea/thiourea derivatives as anti-hyperglycaemic agents and aldose reductase inhibitors.
AID1335662Antidiabetic activity in STZ-induced diabetic Sprague-Dawley rat model assessed as aldose reductase activity at 50 uM//kg, po administered for 8 weeks (Rvb = 44.66 +/- 2.7 U)2016European journal of medicinal chemistry, Nov-29, Volume: 124Design and synthesis of chiral 2H-chromene-N-imidazolo-amino acid conjugates as aldose reductase inhibitors.
AID184013In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-6 M concentration1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID1335654Inhibition of rat lenses ALR2 using DL-glyceraldehyde as substrate preincubated for 10 mins followed by substrate addition measured for 4 mins2016European journal of medicinal chemistry, Nov-29, Volume: 124Design and synthesis of chiral 2H-chromene-N-imidazolo-amino acid conjugates as aldose reductase inhibitors.
AID179748In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-5 M concentration1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID34476Inhibition of aldose reductase in partially purified bovine lens preparation at 10e-7 M concentration1989Journal of medicinal chemistry, Nov, Volume: 32, Issue:11
Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat.
AID230205Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W20Y)2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.
AID181877In vivo galactitol inhibitory activity measured by its ability to inhibit galactitol accumulation in sciatic nerve at 4 mg/Kg/day1992Journal of medicinal chemistry, Nov-27, Volume: 35, Issue:24
Novel spirosuccinimides with incorporated isoindolone and benzisothiazole 1,1-dioxide moieties as aldose reductase inhibitors and antihyperglycemic agents.
AID489642Selectivity ratio of IC50 for human ALR to IC50 for human AR2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
AID170137Compound was evaluated for its ability to reduce carrageenan induced inflammation of rat paw and activity relative to phenylbutazone was reported; Not tested1986Journal of medicinal chemistry, Nov, Volume: 29, Issue:11
Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids.
AID34974The compound was tested for the inhibition of Aldose reductase in rat lens assay.1991Journal of medicinal chemistry, Jul, Volume: 34, Issue:7
Relative structure-inhibition analyses of the N-benzoyl and N-(phenylsulfonyl) amino acid aldose reductase inhibitors.
AID159820Inhibitory activity against human placental aldose reductase (HPAR) with glyceraldehyde as substrate1989Journal of medicinal chemistry, Jun, Volume: 32, Issue:6
Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors.
AID408837Dissociation constant, pKa of the compound2008Bioorganic & medicinal chemistry, Jun-01, Volume: 16, Issue:11
Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives.
AID26074pKa in DMF/H2O was measured1988Journal of medicinal chemistry, Jan, Volume: 31, Issue:1
Spiro hydantoin aldose reductase inhibitors.
AID1204830Inhibition of ALR2 in calf lenses using DL-glyceraldehyde as substrate treated with compound for 10 mins prior to substrate addition by UV spectrophotometer analysis2015European journal of medicinal chemistry, Jun-15, Volume: 98Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones.
AID1143291Inhibition of IFN-gamma/histamine-induced NF-kappaB activation in human NCTC-2544 cells assessed as inhibition of nuclear translocation at 10 uM after 48 hrs by Western blot analysis relative to sorbinil2014European journal of medicinal chemistry, Jun-23, Volume: 81Structure-activity relationships and molecular modelling of new 5-arylidene-4-thiazolidinone derivatives as aldose reductase inhibitors and potential anti-inflammatory agents.
AID34805In vitro inhibitory activity of compound against rat lens aldose reductase2004Journal of medicinal chemistry, May-06, Volume: 47, Issue:10
[1-(3,5-difluoro-4-hydroxyphenyl)-1H-pyrrol-3-yl]phenylmethanone as a bioisostere of a carboxylic acid aldose reductase inhibitor.
AID1143289Inhibition of bovine aldose reductase assessed as oxidation of NADPH2014European journal of medicinal chemistry, Jun-23, Volume: 81Structure-activity relationships and molecular modelling of new 5-arylidene-4-thiazolidinone derivatives as aldose reductase inhibitors and potential anti-inflammatory agents.
AID1478798Inhibition of Sprague-Dawley rat kidney ALR1 using sodium D-glucuronate as substrate by spectrophotometric method2017Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12
N-(Aroyl)-N-(arylmethyloxy)-α-alanines: Selective inhibitors of aldose reductase.
AID34201Inhibitory Activity against Human recombinant Aldose Reductase (wild type)2000Journal of medicinal chemistry, Mar-23, Volume: 43, Issue:6
Molecular modeling of the aldose reductase-inhibitor complex based on the X-ray crystal structure and studies with single-site-directed mutants.
AID34814Inhibition of aldose reductase from rat lens. Value ranges from 0.07 - 1.21989Journal of medicinal chemistry, May, Volume: 32, Issue:5
Synthesis and in vitro aldose reductase inhibitory activity of compounds containing an N-acylglycine moiety.
AID242590Inhibitory concentration against human ALR1 Aldehyde reductase using DL-glyceraldehyde2005Journal of medicinal chemistry, Aug-25, Volume: 48, Issue:17
Structure of aldehyde reductase holoenzyme in complex with the potent aldose reductase inhibitor fidarestat: implications for inhibitor binding and selectivity.
AID1589443Inhibition of rat kidney ALR1 using DL-glyceraldehyde as substrate and NADPH preincubated for 5 mins followed by substrate addition and measured for 30 mins at 2 mins interval by spectrophotometry relative to control2019European journal of medicinal chemistry, Apr-15, Volume: 168Synthesis of new arylsulfonylspiroimidazolidine-2',4'-diones and study of their effect on stimulation of insulin release from MIN6 cell line, inhibition of human aldose reductase, sorbitol accumulations in various tissues and oxidative stress.
AID184011In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-5 M concentration1991Journal of medicinal chemistry, Aug, Volume: 34, Issue:8
Syntheses of tolrestat analogues containing additional substituents in the ring and their evaluation as aldose reductase inhibitors. Identification of potent, orally active 2-fluoro derivatives.
AID34803Concentration required to produce 50% inhibition of aldose reductase enzyme (the literature IC50 value for sorbinil is 0.07 uM)1987Journal of medicinal chemistry, Sep, Volume: 30, Issue:9
Novel inhibitors of rat lens aldose reductase: N-[[(substituted amino)phenyl]sulfonyl]glycines.
AID489638Inhibition of N-terminal 6His-tagged human aldose reductase expressed in Escherichia coli BL21(DE3) mediated NADPH linked pyridine-3-aldehyde reduction2010Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7
Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10.
AID765046Inhibition of partially purified Fischer-344 rat lens ALR2 using D,L-glyceraldehyde as substrate assessed as NADPH consumption by spectrophotometry2013Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue:17
1-Hydroxypyrazole as a bioisostere of the acetic acid moiety in a series of aldose reductase inhibitors.
AID255041In vitro inhibitroy concentration against Aldose reductase incubated at 24 degree C for 15 minutes in pH 7.02005Journal of medicinal chemistry, Oct-06, Volume: 48, Issue:20
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
AID35132The compound was tested for Inhibitory effect against Aldose reductase 1 in bovine kidneys1999Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11
1-Benzopyran-4-one antioxidants as aldose reductase inhibitors.
AID184950Tested in vivo for ability to inhibit sorbitol formation in the lens of a streptozotocinized rat model after oral administration at the dose of 0.75 mg/Kg1990Journal of medicinal chemistry, Jul, Volume: 33, Issue:7
Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID504749qHTS profiling for inhibitors of Plasmodium falciparum proliferation2011Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043
Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets.
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347151Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1347410qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library2019Cellular signalling, 08, Volume: 60A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening.
AID1347405qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347059CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347058CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1347057CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation2019PloS one, , Volume: 14, Issue:7
Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors.
AID1346211Human aldo-keto reductase family 1 member B (1.-.-.- Oxidoreductases)2000Journal of medicinal chemistry, Jun-15, Volume: 43, Issue:12
A potent aldose reductase inhibitor, (2S,4S)-6-fluoro-2', 5'-dioxospiro[chroman-4,4'-imidazolidine]-2-carboxamide (Fidarestat): its absolute configuration and interactions with the aldose reductase by X-ray crystallography.
AID1797505In Vitro Aldose Reductase Inhibition Assay from Article 10.1021/jm034065z: \\A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2003Journal of medicinal chemistry, Jun-05, Volume: 46, Issue:12
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
AID1802103IC50-Activity Assay (AR) from Article 10.1021/acschembio.6b00382: \\IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors\\
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).2014Journal of biomolecular screening, Jul, Volume: 19, Issue:6
A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum.
AID1794808Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL).
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (485)

TimeframeStudies, This Drug (%)All Drugs %
pre-1990203 (41.86)18.7374
1990's152 (31.34)18.2507
2000's75 (15.46)29.6817
2010's43 (8.87)24.3611
2020's12 (2.47)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials44 (8.80%)5.53%
Reviews29 (5.80%)6.00%
Case Studies3 (0.60%)4.05%
Observational0 (0.00%)0.25%
Other424 (84.80%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research Highlights

Safety/Toxicity (3)

ArticleYear
Aldose reductase prevents aldehyde toxicity in cultured human lens epithelial cells.
Experimental eye research, Volume: 83, Issue: 2
2006
Aldose reductase-catalyzed reduction of acrolein: implications in cyclophosphamide toxicity.
Molecular pharmacology, Volume: 45, Issue: 4
1994
An in vitro study of the microsomal metabolism and cellular toxicity of phenytoin, sorbinil and mianserin.
British journal of clinical pharmacology, Volume: 26, Issue: 5
1988
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Long-term Use (2)

ArticleYear
Aldose reductase inhibitors in clinical practice. Preliminary studies on diabetic neuropathy and retinopathy.
Drugs, Volume: 32 Suppl 2
1986
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Pharmacokinetics (2)

ArticleYear
Sorbinil pharmacokinetics in male and female elderly volunteers.
British journal of clinical pharmacology, Volume: 23, Issue: 4
1987
The role of polyols in cerebral cell volume regulation in hypernatremic and hyponatremic states.
Life sciences, Volume: 49, Issue: 9
1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioavailability (7)

ArticleYear
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Molecular pharmacology, Volume: 96, Issue: 5
2019
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
The Journal of biological chemistry, 11-15, Volume: 294, Issue: 46
2019
1-Hydroxypyrazole as a bioisostere of the acetic acid moiety in a series of aldose reductase inhibitors.
Bioorganic & medicinal chemistry, Sep-01, Volume: 21, Issue: 17
2013
A novel series of non-carboxylic acid, non-hydantoin inhibitors of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran-2-sulfonyl)-2H-pyridazin-3-one and congeners.
Journal of medicinal chemistry, Oct-06, Volume: 48, Issue: 20
2005
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
Journal of medicinal chemistry, Jun-05, Volume: 46, Issue: 12
2003
In vivo pharmacokinetics of aldose reductase inhibitors: 3-fluoro-3-deoxy-D-glucose NMR studies in rat brains.
NMR in biomedicine, Volume: 2, Issue: 1
1989
Novel, potent aldose reductase inhibitors: 3,4-dihydro-4-oxo-3-[[5-(trifluoromethyl)-2-benzothiazolyl] methyl]-1-phthalazineacetic acid (zopolrestat) and congeners.
Journal of medicinal chemistry, Volume: 34, Issue: 1
1991
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Dosage (7)

ArticleYear
Inhibition of naphthalene cataract in rats by aldose reductase inhibitors.
Current eye research, Volume: 15, Issue: 4
1996
Kinetics of an orally absorbed aldose reductase inhibitor, sorbinil.
Clinical pharmacology and therapeutics, Volume: 30, Issue: 5
1981
Red blood cell sorbitol as an indicator of polyol pathway activity. Inhibition by sorbinil in insulin-dependent diabetic subjects.
Diabetes, Volume: 33, Issue: 1
1984
Drug-protein conjugates--XVI. Studies of sorbinil metabolism: formation of 2-hydroxysorbinil and unstable protein conjugates.
Biochemical pharmacology, Feb-15, Volume: 37, Issue: 4
1988
Sorbinil pharmacokinetics in male and female elderly volunteers.
British journal of clinical pharmacology, Volume: 23, Issue: 4
1987
Effects of aldose reductase inhibition on the retina and health indices of streptozotocin-diabetic rats.
Documenta ophthalmologica. Advances in ophthalmology, Volume: 64, Issue: 4
1986
A randomized trial of sorbinil, an aldose reductase inhibitor, in diabetic retinopathy. Sorbinil Retinopathy Trial Research Group.
Archives of ophthalmology (Chicago, Ill. : 1960), Volume: 108, Issue: 9
1990
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]