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]
| ID Source | ID |
|---|---|
| PubMed CID | 337359 |
| CHEMBL ID | 266497 |
| CHEBI ID | 102029 |
| SCHEMBL ID | 48877 |
| MeSH ID | M0086766 |
| 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 |
Sorbil is a potent inhibitor of aldose reductase (the first enzyme in the polyol pathway) Sorbinil has been shown to normalize sorbitol levels in relevant tissues.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Sorbinil is an effective ARI, which could play therapeutic role in treating diabetes and diabetic complications. " | ( Sorbinil, an Aldose Reductase Inhibitor, in Fighting Against Diabetic Complications. Huang, Q; Liu, Q; Ouyang, D, 2019) | 3.4 |
| "Sorbinil is a hydantoin aldose reductase inhibitor that has shown promise as therapy for patients with diabetic complications such as neuropathy and retinopathy. " | ( In-vitro assessment of a hypersensitivity syndrome associated with sorbinil. Cannon, M; Gunderson, K; Hutson, NJ; Shear, NH; Spielberg, SP, 1991) | 1.96 |
| "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." | ( Applicability of red blood cell sorbitol measurements to monitor the clinical activity of sorbinil. Aldinger, CE; Just, LJ; Malone, JI; Page, MG; Peterson, MJ, 1986) | 1.21 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Sorbinil has no significant effect on the above metabolites in the normal rat lens." | ( The effect of an aldose reductase inhibitor (Sorbinil) on the level of metabolites in lenses of diabetic rats. Gonzalez, AM; McLean, P; Sochor, M, 1983) | 1.25 |
Sorbil treatment (40 mg/kg) decreased the lens content of sorbitol. Sorbinil treatment also induced functional recovery in myocardial fractional shortening in vivo and preserved contractile function of isolated perfused hearts.
| Excerpt | Reference | Relevance |
|---|---|---|
| "Sorbinil treatment also induced functional recovery in myocardial fractional shortening in vivo and preserved contractile function of isolated perfused hearts." | ( Endotoxin-induced cardiomyopathy and systemic inflammation in mice is prevented by aldose reductase inhibition. Bhatnagar, A; DiMaio, JM; Horton, JW; Ramana, KV; Srivastava, D; Srivastava, SK; White, MD; Willis, MS, 2006) | 1.06 |
| "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." | ( The effect of an aldose reductase inhibitor (Sorbinil) on the level of metabolites in lenses of diabetic rats. Gonzalez, AM; McLean, P; Sochor, M, 1983) | 1.25 |
| "Sorbinil treatment at 20 mg ." | ( Myo-inositol and sorbitol metabolism in relation to peripheral nerve function in experimental diabetes in the rat: the effect of aldose reductase inhibition. Gillon, KR; Hawthorne, JN; Tomlinson, DR, 1983) | 0.99 |
| "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." | ( myo-Inositol and sorbitol in erythrocytes from diabetic patients before and after sorbinil treatment. Lomecky-Janousek, MZ; Popp-Snijders, C; Schouten, JA; van der Veen, EA, 1984) | 1.21 |
| "Sorbinil treatment for 4 wk reduced sciatic nerve sorbitol concentration and improved motor nerve conduction velocity in diabetes of 2-9 mo duration." | ( The effect of aldose reductase inhibition on motor nerve conduction velocity in diabetic rats. Hanwell, MA; Satchell, PM; Turtle, JR; Yue, DK, 1982) | 0.99 |
| "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." | ( Acetyl-L-carnitine corrects the altered peripheral nerve function of experimental diabetes. Benford, S; Korthals, J; Lowitt, S; Malone, JI; Salem, AF, 1995) | 1.01 |
| "Ten sorbinil-treated patients showed significant improvement in axo-glial dysjunction, a characteristic lesion of the node of Ranvier." | ( Overt diabetic neuropathy: repair of axo-glial dysjunction and axonal atrophy by aldose reductase inhibition and its correlation to improvement in nerve conduction velocity. Bril, V; Greene, DA; Nathaniel, V; Prashar, A; Sima, AA; Werb, MR, 1993) | 0.77 |
| "Sorbinil treatment prevented sorbitol accumulation in erythrocytes and tended to have a similar effect in renal cortex, but had no beneficial effect on renal structure or albuminuria." | ( Aldose reductase and the development of renal disease in diabetic dogs. Engerman, RL; Kern, TS, ) | 0.85 |
| "Sorbinil treatment did, however, alter responses of control left and right atria in a manner similar to diabetes." | ( The effects of streptozotocin-induced diabetes and aldose reductase inhibition with sorbinil, on left and right atrial function in the rat. Chess-Williams, R; Sellers, DJ, 2000) | 1.25 |
| "Sorbinil treatment essentially corrected diabetes-induced sorbitol and fructose accumulation, myo-inositol depletion, decrease in free cytosolic NAD+:NADH ratio and energy deficiency." | ( Evaluation of an aldose reductase inhibitor on lens metabolism, ATPases and antioxidative defense in streptozotocin-diabetic rats: an intervention study. Fathallah, L; Obrosova, IG, 2000) | 1.03 |
| "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." | ( The effect of sorbinil, an aldose reductase inhibitor, on aortic function in control and streptozotocin-induced diabetic rats. Chess-Williams, R; Sellers, DJ, 2000) | 1.18 |
| "Sorbinil treatment completely prevented renal cortical sorbital accumulation, but did not abolish kidney enlargement or the increase in ultrafiltration pressure and glomerular filtration rate." | ( Sorbinil does not prevent hyperfiltration, elevated ultrafiltration pressure and albuminuria in streptozotocin-diabetic rats. Aperia, A; Celsi, G; Eklöf, AC; Körner, A; Linné, T; Persson, B, 1992) | 2.45 |
| "Sorbinil treatment was continued throughout the hyper- and hyponatremic periods." | ( The role of polyols in cerebral cell volume regulation in hypernatremic and hyponatremic states. Futterweit, S; Hammer, E; Oates, P; Siegel, TW; Trachtman, H, 1991) | 1 |
| "Sorbinil treatment markedly reduced or completely prevented all of these changes in galactose-fed, as well as in diabetic rats." | ( Vascular filtration function in galactose-fed versus diabetic rats: the role of polyol pathway activity. Chang, K; Kilo, C; Province, MA; Pugliese, G; Speedy, A; Tilton, RG; Williamson, JR, 1990) | 1 |
| "Sorbinil treatment completely abolished the formation of this protein." | ( Non-tryptophan fluorescence and high molecular weight protein formation in lens crystallins of rats with chronic galactosemia: prevention by the aldose reductase inhibitor sorbinil. Monnier, VM; Nagaraj, RH, 1990) | 1.19 |
| "Sorbinil treatment of diabetic animals was associated with normalization of both lens sorbitol and taurine levels." | ( Nonosmotic diabetic cataracts. Cook, WR; Lowitt, S; Malone, JI, 1990) | 1 |
| "Sorbinil treatment prevented approximately 70% of the increase in total protein excretion despite persistent hyperglycemia, glycosuria and ketonuria." | ( Diminished proteinuria in diabetes mellitus by sorbinil, an aldose reductase inhibitor. Beyer-Mears, A; Cruz, E; Edelist, T; Varagiannis, E, 1986) | 1.25 |
| "Sorbinil treatment prevented the 10-fold increase in nerve sorbitol found with diabetes." | ( The effects of sorbinil on peripheral nerve conduction velocity, polyol concentrations and morphology in the streptozotocin-diabetic rat. Cameron, NE; Leonard, MB; Ross, IS; Whiting, PH, 1986) | 1.35 |
| "Sorbinil treatment failed to improve even slightly the abnormalities in cellular replication induced by high glucose." | ( The polyol pathway and glucose 6-phosphate in human endothelial cells cultured in high glucose concentrations. Boss, GR; Lane, MJ; Lorenzi, M; Montisano, DF; Toledo, S, 1987) | 0.99 |
| "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." | ( Increased nerve polyol levels in experimental diabetes and their reversal by Sorbinil. Ross, IS; Whiting, PH, 1988) | 1.23 |
| "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." | ( Endotoxin-induced cardiomyopathy and systemic inflammation in mice is prevented by aldose reductase inhibition. Bhatnagar, A; DiMaio, JM; Horton, JW; Ramana, KV; Srivastava, D; Srivastava, SK; White, MD; Willis, MS, 2006) | 0.67 |
| "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." | ( Prevention and reversal of defective axonal transport and motor nerve conduction velocity in rats with experimental diabetes by treatment with the aldose reductase inhibitor Sorbinil. Mayer, JH; Moriarty, RJ; Tomlinson, DR, 1984) | 0.8 |
| "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." | ( The effects of streptozotocin-induced diabetes and aldose reductase inhibition with sorbinil, on left and right atrial function in the rat. Chess-Williams, R; Sellers, DJ, 2000) | 0.85 |
| "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." | ( Altered neuroexcitability in experimental diabetic neuropathy: effect of acetyl-L-carnitine. Corsico, N; Lowitt, S; Malone, JI; Orfalian, Z, 1992) | 0.62 |
| "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." | ( Evaluation of the effect of aldose reductase inhibition on increased basement membrane collagen fluorescence in diabetic rats. Cohen, MP; Klepser, H; Wu, VY, 1991) | 0.6 |
| Excerpt | Reference | Relevance |
|---|---|---|
| "Acrolein, a highly cytotoxic aldehyde, is a metabolic by-product of the antineoplastic agent cyclophosphamide and is responsible for the development of hemorrhagic cystitis, a serious side effect of cyclophosphamide therapy." | ( Aldose reductase-catalyzed reduction of acrolein: implications in cyclophosphamide toxicity. Hunsaker, LA; Kolb, NS; Vander Jagt, DL, 1994) | 0.29 |
| " We have shown earlier that aldose reductase (AR) besides reducing glucose to sorbitol, efficiently reduces various toxic lipid-derived aldehydes, generated under oxidative stress, with K(m) in the physiological range." | ( Aldose reductase prevents aldehyde toxicity in cultured human lens epithelial cells. Ansari, NH; Pladzyk, A; Ramana, KV; Srivastava, SK, 2006) | 0.33 |
| Excerpt | Reference | Relevance |
|---|---|---|
| " Elimination half-life tended to be longer in males than in females." | ( Sorbinil pharmacokinetics in male and female elderly volunteers. Petrie, JC; Scott, AK; Webster, J, 1987) | 1.72 |
Oral sorbinil (5 mg/kg) dramatically reduced (80-90%) sorbitol levels in tissues without affecting blood glucose. The RBC dose-response curve was similar to that in lens and sciatic nerve. Chronic dosing with Sorbinil induced 2-hydroxylation of the drug.
| Excerpt | Relevance | Reference |
|---|---|---|
| " On the basis of these results, it is unlikely that sorbinil administered at a dosage of 250 mg daily for 3 years has a clinically important effect on the course of retinopathy in adults with insulin-dependent diabetes of moderate duration." | ( A randomized trial of sorbinil, an aldose reductase inhibitor, in diabetic retinopathy. Sorbinil Retinopathy Trial Research Group. , 1990) | 0.84 |
| " Chronic dosing with sorbinil (150 mg/kg x 5) induced 2-hydroxylation of the drug, the 0-24 hr urinary excretion of 2HSB increasing from 17." | ( Drug-protein conjugates--XVI. Studies of sorbinil metabolism: formation of 2-hydroxysorbinil and unstable protein conjugates. Maggs, JL; Park, BK, 1988) | 0.86 |
| " In diabetic rats with severe hyperglycemia, oral sorbinil (5 mg/kg) dramatically reduced (80-90%) sorbitol levels in tissues without affecting blood glucose; the RBC dose-response curve was similar to that in lens and sciatic nerve." | ( Red blood cell sorbitol as an indicator of polyol pathway activity. Inhibition by sorbinil in insulin-dependent diabetic subjects. Aldinger, CE; Leavengood, H; Malone, JI; O'Brien, MM; Page, MG; Peterson, MJ, 1984) | 0.75 |
| " It was found that at the same dosage of 10 mg/kg/day, both AL01576 and AL04114 completely prevented all morphological and biochemical changes in the lenses of naphthalene-fed rats." | ( Inhibition of naphthalene cataract in rats by aldose reductase inhibitors. Lou, MF; Xu, GT; York, B; Zigler, S, 1996) | 0.29 |
| Role | Description |
|---|---|
| EC 1.1.1.21 (aldehyde reductase) inhibitor | An 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). |
| antioxidant | A 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] | |
| Class | Description |
|---|---|
| chromanes | |
| oxaspiro compound | A spiro compound in which at least one of the cyclic components is an oxygen heterocyle. |
| azaspiro compound | An azaspiro compound is a spiro compound in which at least one of the cyclic components is a nitrogen heterocyle. |
| organofluorine compound | An organofluorine compound is a compound containing at least one carbon-fluorine bond. |
| imidazolidinone | An 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 | Taxonomy | Measurement | Average (µ) | Min (ref.) | Avg (ref.) | Max (ref.) | Bioassay(s) |
|---|---|---|---|---|---|---|---|
| RAR-related orphan receptor gamma | Mus musculus (house mouse) | Potency | 33.4915 | 0.0060 | 38.0041 | 19,952.5996 | AID1159521 |
| Microtubule-associated protein tau | Homo sapiens (human) | Potency | 8.9125 | 0.1800 | 13.5574 | 39.8107 | AID1468 |
| AR protein | Homo sapiens (human) | Potency | 29.7629 | 0.0002 | 21.2231 | 8,912.5098 | AID743042; AID743054; AID743063 |
| ATP-dependent phosphofructokinase | Trypanosoma brucei brucei TREU927 | Potency | 35.4813 | 0.0601 | 10.7453 | 37.9330 | AID492961 |
| [prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023] | |||||||
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID182013 | Compound was evaluated in vivo for the inhibition of sorbitol accumulation administered orally at a dose of 0.25 mg/kg. | 1991 | Journal 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. |
| AID34506 | Inhibitory activity against bovine lens aldose reductase | 1985 | Journal of medicinal chemistry, Nov, Volume: 28, Issue:11 | Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil. |
| AID34804 | In vitro inhibitory activity against aldose reductase (ALR2) from rat lens extraction. | 2003 | Journal 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. |
| AID489641 | Selectivity ratio of IC50 for human ALR to IC50 for AKR1B10 | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10. |
| AID1589440 | Inhibition 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 t | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Synthesis 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. |
| AID34788 | In vitro inhibition of rabbit lens aldose reductase at 10e-5 M. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
| AID34799 | Compound was tested for its ability to inhibit crude aldose reductase obtained from rat lens | 1986 | Journal 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. |
| AID34653 | Inhibitory activity against human placental aldose reductase in Sepharose 4B column at day 7 | 1985 | Journal 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. |
| AID184947 | Tested 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/Kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID34970 | Inhibitory concentration against aldose reductase obtained from rat lens | 1989 | Journal of medicinal chemistry, Jan, Volume: 32, Issue:1 | N- and 2-substituted N-(phenylsulfonyl)glycines as inhibitors of rat lens aldose reductase. |
| AID241413 | Inhibitory concentration against human ALR2 | 2005 | Journal 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. |
| AID230202 | Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W111A) | 2000 | Journal 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. |
| AID233810 | The ratio of the inhibitory concentration causing a 50% reduction of sorbitol in the isolated nerve to the IC50 in the isolated enzyme | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Spiro hydantoin aldose reductase inhibitors. |
| AID232928 | Selectivity as ratio of IC50 for rat lens and kidney aldose reductase | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors. |
| AID220720 | In vitro inhibitory activity against human recombinant Aldose reductase in streptozotocin diabetic rat at 50 mg/kg | 2003 | Journal 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. |
| AID241371 | Inhibitory concentration against rat ALR2 aldose reductase | 2005 | Journal 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. |
| AID1315347 | In 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 staining | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Characterization of Emodin as a Therapeutic Agent for Diabetic Cataract. |
| AID1478797 | Inhibition 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 method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | N-(Aroyl)-N-(arylmethyloxy)-α-alanines: Selective inhibitors of aldose reductase. |
| AID381848 | Inhibition of aldose reductase in rat lenses | 2008 | Bioorganic & medicinal chemistry, Apr-01, Volume: 16, Issue:7 | Design and synthesis of N-(3,5-difluoro-4-hydroxyphenyl)benzenesulfonamides as aldose reductase inhibitors. |
| AID1589441 | Inhibition 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 control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Synthesis 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. |
| AID1066260 | Inhibition of AKR1B1 in mouse RAW264.7 cells assessed as inhibition of sorbitol accumulation after 24 hrs by colorimetric assay | 2014 | Journal 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. |
| AID177265 | Compound was evaluated for the ED50(chronic) in male Sprague-Dawley rats(n=4) treated with streptozotocin (85 mg/kg intravenously). | 1991 | Journal 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. |
| AID182014 | Compound was evaluated in vivo for the inhibition of sorbitol accumulation administered orally at a dose of 0.75 mg/kg. | 1991 | Journal 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. |
| AID322411 | Inhibition of mouse recombinant AKR1C21 at 50 uM | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors. |
| AID1315351 | In 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%) | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Characterization of Emodin as a Therapeutic Agent for Diabetic Cataract. |
| AID203729 | Inhibition of sorbitol dehydrogenase from sheep liver (40 U/mg of protein) | 1996 | Journal 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. |
| AID34354 | In vitro aldose reductase inhibitory activity measured by NADPH-dependent inhibition of glyceraldehyde reduction in a partially purified bovine lens preparation at 10E-6 M | 1992 | Journal 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. |
| AID184331 | In vivo galactitol inhibitory activity measured by its ability to inhibit galactitol accumulation in diaphragm at 4 mg/Kg/day | 1992 | Journal 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. |
| AID75435 | Evaluated for inhibition of glutathione reductase.; No inhibition | 1996 | Journal 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. |
| AID379162 | Inhibition of human recombinant ALR2 | 2006 | Journal of natural products, Oct, Volume: 69, Issue:10 | Phenolic marine natural products as aldose reductase inhibitors. |
| AID182432 | In vivo inhibition of galactitol accumulation in the sciatic nerves of rat at a dose of 4 mg/kg/day | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat. |
| AID184961 | Tested 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/kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID34798 | Compound was tested for inhibitory concentration against rat lens aldose reductase (uncompetitive inhibition type) | 1986 | Journal of medicinal chemistry, Jun, Volume: 29, Issue:6 | Synthesis and rat lens aldose reductase inhibitory activity of some benzopyran-2-ones. |
| AID309933 | Inhibition of aldose reductase | 2007 | Bioorganic & 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. |
| AID34964 | Inhibitory activity measured against rat lens aldose reductase using 3-pyridinecarboxaldehyde as substrate | 1991 | Journal 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. |
| AID468476 | Inhibition of Albino rat eye lens ALR2 assessed as NADPH oxidation by spectrophotometry | 2010 | European 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. |
| AID34637 | In vitro inhibitory activity against recombinant human aldose reductase (ALR2) was determined | 2003 | Journal 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. |
| AID549694 | Inhibition of bovine lens aldose reductase assessed as inhibition of NDAPH oxidation by non-linear regression analysis | 2011 | Bioorganic & medicinal chemistry letters, Jan-01, Volume: 21, Issue:1 | In vitro evaluation of 5-arylidene-2-thioxo-4-thiazolidinones active as aldose reductase inhibitors. |
| AID35109 | In vitro inhibitory activity against aldose reductase of rat lens at 2.5x10E-7 M concentration | 2003 | Journal 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. |
| AID537153 | Inhibition of rat lens ALR2 | 2010 | Journal 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. |
| AID489639 | Inhibition of N-terminal 6His-tagged human aldehyde reductase expressed in Escherichia coli BL21(DE3) mediated D-glucuronate reduction | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10. |
| AID34355 | In vitro aldose reductase inhibitory activity measured by NADPH-dependent inhibition of glyceraldehyde reduction in a partially purified bovine lens preparation at 10E-7 M | 1992 | Journal 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. |
| AID34654 | Inhibitory activity against human placental aldose reductase in Sepharose 4B column at time 1 | 1985 | Journal 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. |
| AID1700253 | Inhibition of ALR2 (unknown origin) | 2020 | Bioorganic & medicinal chemistry letters, 12-15, Volume: 30, Issue:24 | Synthesis and biological screening of thiosemicarbazones of substituted 3-acetylcoumarins having d-glucose moiety. |
| AID177556 | Ability to cause 50% reduction in sorbitol levels of sciatic nerve of streptozotocinized rats was determined | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Spiro hydantoin aldose reductase inhibitors. |
| AID34965 | Inhibitory activity against aldose reductase in rat lens | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Relative structure-inhibition analyses of the N-benzoyl and N-(phenylsulfonyl) amino acid aldose reductase inhibitors. |
| AID34655 | Tested for in vitro inhibition activity against human Aldose reductase (human AR) | 2000 | Journal 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. |
| AID1589444 | Selectivity ratio of IC50 for rat kidney ALR1 IC50 to IC50 for human recombinant ALR2 | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Synthesis 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. |
| AID35113 | In vitro percentage inhibition of rat lens aldose reductase at 10E-6 M concentration | 2004 | Journal 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. |
| AID184964 | Tested 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/Kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID322413 | Inhibition of human recombinant aldose reductase | 2008 | Bioorganic & medicinal chemistry, Mar-15, Volume: 16, Issue:6 | Inhibition of 3(17)alpha-hydroxysteroid dehydrogenase (AKR1C21) by aldose reductase inhibitors. |
| AID35133 | Compound was tested for Ratio of IC50(ALR1)/(ALR2) | 1999 | Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11 | 1-Benzopyran-4-one antioxidants as aldose reductase inhibitors. |
| AID462440 | Inhibition of aldose reductase in Fischer-344 rat lens homogenate by spectrometric analysis | 2010 | Bioorganic & 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. |
| AID178946 | Effective dose required to inhibit sorbitol accumulation in sciatic nerves of streptozotocinized rats administered perorally | 1985 | Journal of medicinal chemistry, Nov, Volume: 28, Issue:11 | Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil. |
| AID34641 | Inhibitory activity against human placenta aldose reductase | 1985 | Journal of medicinal chemistry, Nov, Volume: 28, Issue:11 | Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil. |
| AID34786 | In vitro inhibition of rabbit lens aldose reductase at 10e-4 M. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
| AID75439 | In vitro inhibitory activity against glutathione reductase (GR) from bakers yeast; Not active | 2003 | Journal 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. |
| AID34475 | Inhibition of aldose reductase in partially purified bovine lens preparation at 10e-6 M. | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat. |
| AID184953 | Tested 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/Kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID26108 | pKa value for the compound was determined | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Isoxazolidine-3,5-diones as lens aldose reductase inhibitors. |
| AID159818 | Inhibition of human placental aldose reductase (HPAR) activity with glyceraldehyde as substrate | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors. |
| AID1124833 | Inhibition of Fischer-344 rat lens ALR2 using D, L-glyceraldehyde as substrate by spectrophotometry | 2014 | Bioorganic & 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. |
| AID184954 | Tested 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/Kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID34505 | Inhibition of bovine lens aldose reductase with DL-glyceraldehyde as substrate | 1984 | Journal 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. |
| AID35135 | In vitro inhibitory activity against Aldose reductase 2 obtained from calf lenses | 1999 | Journal 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. |
| AID34634 | In vitro inhibitory activity against Aldose reductase isolated from human placenta | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID254230 | Binding constant against wild-type human aldose reductase at 18.9 uM | 2005 | Journal 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. |
| AID1589442 | Inhibition 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 control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Synthesis 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. |
| AID34650 | Inhibitory activity against human placental aldose reductase in Orange A column at day 8 | 1985 | Journal 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. |
| AID34646 | Inhibitory activity against human placental aldose reductase in 30 -70% (NH4)2SO4. | 1985 | Journal 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. |
| AID230203 | Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W111Y). | 2000 | Journal 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. |
| AID34969 | Inhibitory concentration to aldose reductase (ALR-2) obtained from rat lens | 2001 | Journal 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. |
| AID179749 | In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-6 M concentration | 1991 | Journal 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. |
| AID462442 | Inhibition of aldose reductase | 2010 | Bioorganic & 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. |
| AID182579 | In vivo inhibition of sorbitol accumulation in rat sciatic nerves at 10e-5 M concentration | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat. |
| AID194291 | Compound was evaluated in vivo for percent inhibition of polyol accumulation at a dose of 3 mg/kg per day. | 1992 | Journal 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. |
| AID477037 | Inhibition of aldose reductase | 2010 | European 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. |
| AID34975 | In vitro inhibition of Aldose reductase (AR) from rat lens (RL) | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors. |
| AID1443999 | Inhibition of Fischer-344 rat lens ALR2 | 2017 | European journal of medicinal chemistry, Apr-21, Volume: 130 | Enhancing activity and selectivity in a series of pyrrol-1-yl-1-hydroxypyrazole-based aldose reductase inhibitors: The case of trifluoroacetylation. |
| AID1315345 | In 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 staining | 2016 | Journal of natural products, 05-27, Volume: 79, Issue:5 | Characterization of Emodin as a Therapeutic Agent for Diabetic Cataract. |
| AID107292 | Compound was evaluated for its analgesic activity in mice by mouse phenylquinone writhing assay, and the activity relative to aspirin was reported; Not tested | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
| AID603256 | Inhibition of bovine lens ALR2 | 2011 | European 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. |
| AID203732 | In vitro inhibitory activity against sorbitol dehydrogenase (SD) from sheep liver; Not active | 2003 | Journal 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. |
| AID182593 | In vivo inhibition of sorbitol accumulation in rat sciatic nerves at 5*10e-6 M concentration | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat. |
| AID489631 | Inhibition of reductase activity of N-terminal 6His-tagged AKR1B10 expressed in Escherichia coli BL21(DE3) assessed as inhibition of NADPH linked pyridine-3-aldehyde reduction | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10. |
| AID34783 | Tested in vitro for inhibitory activity against partially purified aldose reductase from male rabbit lens | 1992 | Journal 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. |
| AID35136 | Inhibition of Aldose reductase 2 of bovine lens | 1999 | Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11 | 1-Benzopyran-4-one antioxidants as aldose reductase inhibitors. |
| AID34177 | Tested for in vitro inhibition activity against human aldehyde reductase (AHR) | 2000 | Journal 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. |
| AID230204 | Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W20A). | 2000 | Journal 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. |
| AID34351 | In vitro % decrease of aldose reductase measured in isolated partially purified bovine lens preparations at 10e-7 M concentration | 1991 | Journal 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. |
| AID1646335 | Inhibition of human recombinant AKR1B1 assessed as D,L-glyceraldehyde reduction pretreated with 0.3M DMSO followed by compound addition by DMSO-perturbation assay | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Early identification of promiscuous attributes of aldose reductase inhibitors using a DMSO-perturbation assay. |
| AID34638 | In vitro inhibitory activity towards human placenta aldose reductase | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Spiro hydantoin aldose reductase inhibitors. |
| AID34795 | Inhibition of crude aldose reductase of rat lens | 1986 | Journal of medicinal chemistry, Oct, Volume: 29, Issue:10 | Synthesis and aldose reductase inhibitory activity of substituted 2-oxoquinoline-1-acetic acid derivatives. |
| AID537152 | Inhibition of Fischer-344 rat lens ALR2 at 0.25 uM | 2010 | Journal 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. |
| AID299415 | Inhibition of bovine aldose reductase | 2007 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 17, Issue:14 | Evaluation of in vitro aldose redutase inhibitory activity of 5-arylidene-2,4-thiazolidinediones. |
| AID181496 | 50% reduction in sorbitol accumulation in isolated sciatic nerves incubated in the presence of high glucose concentration | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Spiro hydantoin aldose reductase inhibitors. |
| AID34789 | In vitro inhibition of rabbit lens aldose reductase at 10e-6 M. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
| AID184958 | Tested 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/Kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID241043 | Inhibition of aldose reductase from pig lenses | 2004 | Journal of medicinal chemistry, Oct-07, Volume: 47, Issue:21 | Soft docking and multiple receptor conformations in virtual screening. |
| AID232953 | Inhibitory activity measured against pig kidney aldehyde reductase using 3-pyridinecarboxaldehyde as substrate | 1991 | Journal 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. |
| AID184354 | In vivo galactitol inhibitory activity measured by its ability to inhibit galactitol accumulation in lens at 4 mg/Kg/day | 1992 | Journal 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. |
| AID29166 | Dissociation constant was determined | 2003 | Journal 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. |
| AID184963 | Tested 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/Kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID34664 | Selectivity ratio measured as the IC50 ratio of aldehyde/aldose reductase values | 1991 | Journal 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. |
| AID34210 | In vitro % decrease of aldose reductase was measured in isolated partially purified bovine lens preparations at 10e-6 M concentration | 1991 | Journal 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. |
| AID35115 | Inhibition of rat lens aldose reductase at 50 uM | 1982 | Journal of medicinal chemistry, Jun, Volume: 25, Issue:6 | Isoxazolidine-3,5-diones as lens aldose reductase inhibitors. |
| AID408834 | Inhibition of bovine lens ALR2 assessed as reduction of D,L-glyceraldehyde by spectrophotometry | 2008 | Bioorganic & 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. |
| AID34198 | In vitro inhibitory activity against aldehyde reductase 1 (ALR1) from rat kidney. | 2003 | Journal 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. |
| AID176729 | Dose causing 50% reduction in sorbitol accumulation in isolated sciatic nerves of streptozotocinized rats, (tid) | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Spiro hydantoin aldose reductase inhibitors. |
| AID256543 | Binding constant against Leu300Pro mutant of aldose reductase at 37.8 uM | 2005 | Journal 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. |
| AID34648 | Inhibitory activity against human placental aldose reductase in Orange A column at at time 2 | 1985 | Journal 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. |
| AID35134 | Evaluated for inhibition of Aldose reductase 2 | 1996 | Journal 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. |
| AID182251 | In vivo inhibition of galactitol accumulation in sciatic nerves of rat at 4 mg/kg/day | 1991 | Journal 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. |
| AID34985 | Compound was tested for percent inhibition of aldose reductase inhibitory activity using rat lens assay at concentration of 100 uM; ND= not determined | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Novel inhibitors of rat lens aldose reductase: N-[[(substituted amino)phenyl]sulfonyl]glycines. |
| AID34661 | Inhibitory activity measured against human placental aldose reductase at a concentration of 10e-5 M | 1991 | Journal 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. |
| AID34962 | Inhibitory activity against rat lens aldose reductase | 1985 | Journal of medicinal chemistry, Nov, Volume: 28, Issue:11 | Synthesis, absolute configuration, and conformation of the aldose reductase inhibitor sorbinil. |
| AID1713572 | Inhibition 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 analysis | 2016 | Bioorganic & medicinal chemistry letters, 10-15, Volume: 26, Issue:20 | Pterin-7-carboxamides as a new class of aldose reductase inhibitors. |
| AID93598 | Inhibitory activity on sorbital accumulation in human retinal cells was determined | 2003 | Journal 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. |
| AID488380 | Inhibition of bovine lens aldose reductase | 2010 | Bioorganic & medicinal chemistry, Jun-01, Volume: 18, Issue:11 | Identification of new non-carboxylic acid containing inhibitors of aldose reductase. |
| AID170935 | Compound 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 contents | 1992 | Journal 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. |
| AID242609 | Inhibitory concentration against porcine ALR1 Aldehyde reductase using DL-glyceraldehyde | 2005 | Journal 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. |
| AID34196 | Evaluated for inhibition of Aldehyde reductase 1 | 1996 | Journal 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. |
| AID34782 | In vitro inhibition of rabbit lens aldose reductase. | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
| AID182073 | In vivo inhibition of galactitol accumulation in diaphragm of rat at 4 mg/kg/day | 1991 | Journal 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. |
| AID182408 | In vivo inhibition of galactitol accumulation in the diaphragm of rat at a dose of 4 mg/kg/day | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat. |
| AID35127 | Inhibition of partially purified aldose reductase obtained from rat lens (100 uM ); ND is No Data | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis and in vitro aldose reductase inhibitory activity of compounds containing an N-acylglycine moiety. |
| AID182586 | In vivo inhibition of sorbitol accumulation in rat sciatic nerves at 10e-6 M concentration | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat. |
| AID34178 | Inhibitory activity measured against pig kidney aldehyde reductase using 3-pyridinecarboxaldehyde as substrate | 1991 | Journal 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. |
| AID720961 | Inhibition of Fischer-344 rat lens ALR2 using D-glycuronate as substrate by spectrophotometry | 2013 | Bioorganic & 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. |
| AID1646336 | Inhibition of human recombinant AKR1B1 assessed as D,L-glyceraldehyde reduction pretreated with 0.7M DMSO followed by compound addition by DMSO-perturbation assay | 2020 | Bioorganic & medicinal chemistry letters, 01-15, Volume: 30, Issue:2 | Early identification of promiscuous attributes of aldose reductase inhibitors using a DMSO-perturbation assay. |
| AID194289 | Compound was evaluated in vivo for percent inhibition of polyol accumulation at a dose of 15 mg/kg per day | 1992 | Journal 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. |
| AID178209 | Effective dose of aldose reductase was evaluated by measuring galactitol accumulation in sciatic nerves of rat at 4 mg/kg/day | 1991 | Journal 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. |
| AID34973 | Tested for in vitro inhibition activity against rat Aldose reductase (AR) | 2000 | Journal 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. |
| AID34662 | Inhibitory activity measured against human placental aldose reductase at a concentration of 10e-6 M | 1991 | Journal 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. |
| AID34211 | In vitro % decrease of aldose reductase was measured in isolated partially purified bovine lens preparations at 10e-7 M concentration | 1991 | Journal 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. |
| AID95257 | In vitro inhibitory activity against L-Hexonate Dehydrogenase (L-HDH) from rat kidney (RK) | 1991 | Journal of medicinal chemistry, Nov, Volume: 34, Issue:11 | Spiro[fluoreneisothiazolidin]one dioxides: new aldose reductase and L-hexonate dehydrogenase inhibitors. |
| AID489640 | Selectivity ratio of IC50 for human AR to IC50 for AKR1B10 | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10. |
| AID1142509 | Inhibition of aldose reductase in rat lens by spectrophotometer analysis | 2014 | European journal of medicinal chemistry, Jun-10, Volume: 80 | Synthesis and biological evaluation of some new pyrazoline substituted benzenesulfonylurea/thiourea derivatives as anti-hyperglycaemic agents and aldose reductase inhibitors. |
| AID1335662 | Antidiabetic 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) | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Design and synthesis of chiral 2H-chromene-N-imidazolo-amino acid conjugates as aldose reductase inhibitors. |
| AID184013 | In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-6 M concentration | 1991 | Journal 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. |
| AID1335654 | Inhibition of rat lenses ALR2 using DL-glyceraldehyde as substrate preincubated for 10 mins followed by substrate addition measured for 4 mins | 2016 | European journal of medicinal chemistry, Nov-29, Volume: 124 | Design and synthesis of chiral 2H-chromene-N-imidazolo-amino acid conjugates as aldose reductase inhibitors. |
| AID179748 | In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-5 M concentration | 1991 | Journal 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. |
| AID34476 | Inhibition of aldose reductase in partially purified bovine lens preparation at 10e-7 M concentration | 1989 | Journal of medicinal chemistry, Nov, Volume: 32, Issue:11 | Orally active aldose reductase inhibitors derived from bioisosteric substitutions on tolrestat. |
| AID230205 | Inhibitory Activity ratio (IC50 ratio) calculated by Human recombinant aldose reductase wild type against Mutant Aldose reductase (W20Y) | 2000 | Journal 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. |
| AID181877 | In vivo galactitol inhibitory activity measured by its ability to inhibit galactitol accumulation in sciatic nerve at 4 mg/Kg/day | 1992 | Journal 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. |
| AID489642 | Selectivity ratio of IC50 for human ALR to IC50 for human AR | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10. |
| AID170137 | Compound was evaluated for its ability to reduce carrageenan induced inflammation of rat paw and activity relative to phenylbutazone was reported; Not tested | 1986 | Journal of medicinal chemistry, Nov, Volume: 29, Issue:11 | Antiinflammatory and aldose reductase inhibitory activity of some tricyclic arylacetic acids. |
| AID34974 | The compound was tested for the inhibition of Aldose reductase in rat lens assay. | 1991 | Journal of medicinal chemistry, Jul, Volume: 34, Issue:7 | Relative structure-inhibition analyses of the N-benzoyl and N-(phenylsulfonyl) amino acid aldose reductase inhibitors. |
| AID159820 | Inhibitory activity against human placental aldose reductase (HPAR) with glyceraldehyde as substrate | 1989 | Journal of medicinal chemistry, Jun, Volume: 32, Issue:6 | Rotationally restricted mimics of rigid molecules: nonspirocyclic hydantoin aldose reductase inhibitors. |
| AID408837 | Dissociation constant, pKa of the compound | 2008 | Bioorganic & 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. |
| AID26074 | pKa in DMF/H2O was measured | 1988 | Journal of medicinal chemistry, Jan, Volume: 31, Issue:1 | Spiro hydantoin aldose reductase inhibitors. |
| AID1204830 | Inhibition of ALR2 in calf lenses using DL-glyceraldehyde as substrate treated with compound for 10 mins prior to substrate addition by UV spectrophotometer analysis | 2015 | European journal of medicinal chemistry, Jun-15, Volume: 98 | Synthesis, characterization, hypoglycemic and aldose reductase inhibition activity of arylsulfonylspiro[fluorene-9,5'-imidazolidine]-2',4'-diones. |
| AID1143291 | Inhibition 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 sorbinil | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Structure-activity relationships and molecular modelling of new 5-arylidene-4-thiazolidinone derivatives as aldose reductase inhibitors and potential anti-inflammatory agents. |
| AID34805 | In vitro inhibitory activity of compound against rat lens aldose reductase | 2004 | Journal 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. |
| AID1143289 | Inhibition of bovine aldose reductase assessed as oxidation of NADPH | 2014 | European journal of medicinal chemistry, Jun-23, Volume: 81 | Structure-activity relationships and molecular modelling of new 5-arylidene-4-thiazolidinone derivatives as aldose reductase inhibitors and potential anti-inflammatory agents. |
| AID1478798 | Inhibition of Sprague-Dawley rat kidney ALR1 using sodium D-glucuronate as substrate by spectrophotometric method | 2017 | Bioorganic & medicinal chemistry, 06-15, Volume: 25, Issue:12 | N-(Aroyl)-N-(arylmethyloxy)-α-alanines: Selective inhibitors of aldose reductase. |
| AID34201 | Inhibitory Activity against Human recombinant Aldose Reductase (wild type) | 2000 | Journal 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. |
| AID34814 | Inhibition of aldose reductase from rat lens. Value ranges from 0.07 - 1.2 | 1989 | Journal of medicinal chemistry, May, Volume: 32, Issue:5 | Synthesis and in vitro aldose reductase inhibitory activity of compounds containing an N-acylglycine moiety. |
| AID242590 | Inhibitory concentration against human ALR1 Aldehyde reductase using DL-glyceraldehyde | 2005 | Journal 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. |
| AID1589443 | Inhibition 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 control | 2019 | European journal of medicinal chemistry, Apr-15, Volume: 168 | Synthesis 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. |
| AID184011 | In vitro inhibition of sorbitol accumulation was measured in rat sciatic nerves incubated in the presence of 50 mM glucose at 10e-5 M concentration | 1991 | Journal 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. |
| AID34803 | Concentration required to produce 50% inhibition of aldose reductase enzyme (the literature IC50 value for sorbinil is 0.07 uM) | 1987 | Journal of medicinal chemistry, Sep, Volume: 30, Issue:9 | Novel inhibitors of rat lens aldose reductase: N-[[(substituted amino)phenyl]sulfonyl]glycines. |
| AID489638 | Inhibition of N-terminal 6His-tagged human aldose reductase expressed in Escherichia coli BL21(DE3) mediated NADPH linked pyridine-3-aldehyde reduction | 2010 | Bioorganic & medicinal chemistry, Apr-01, Volume: 18, Issue:7 | Chromene-3-carboxamide derivatives discovered from virtual screening as potent inhibitors of the tumour maker, AKR1B10. |
| AID765046 | Inhibition of partially purified Fischer-344 rat lens ALR2 using D,L-glyceraldehyde as substrate assessed as NADPH consumption by spectrophotometry | 2013 | Bioorganic & 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. |
| AID255041 | In vitro inhibitroy concentration against Aldose reductase incubated at 24 degree C for 15 minutes in pH 7.0 | 2005 | Journal 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. |
| AID35132 | The compound was tested for Inhibitory effect against Aldose reductase 1 in bovine kidneys | 1999 | Journal of medicinal chemistry, Jun-03, Volume: 42, Issue:11 | 1-Benzopyran-4-one antioxidants as aldose reductase inhibitors. |
| AID184950 | Tested 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/Kg | 1990 | Journal of medicinal chemistry, Jul, Volume: 33, Issue:7 | Spiro hydantoin aldose reductase inhibitors derived from 8-aza-4-chromanones. |
| AID1347086 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1296008 | Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening | 2020 | SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1 | Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening. |
| AID1508630 | Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay | 2021 | Cell reports, 04-27, Volume: 35, Issue:4 | A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome. |
| AID1347083 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347091 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347100 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347096 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347108 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347095 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347104 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347101 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347099 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347092 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1745845 | Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347106 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID651635 | Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression | |||
| AID1347097 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347424 | RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
| AID1347082 | qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal | 2020 | Antiviral research, 01, Volume: 173 | A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity. |
| AID1347090 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347093 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347154 | Primary screen GU AMC qHTS for Zika virus inhibitors | 2020 | Proceedings 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. |
| AID1347407 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection | 2020 | ACS 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. |
| AID1347089 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347102 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347425 | Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1) | 2019 | The 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. |
| AID1347107 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347103 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347105 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347094 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID1347098 | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 2018 | Oncotarget, Jan-12, Volume: 9, Issue:4 | Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing. |
| AID504749 | qHTS profiling for inhibitors of Plasmodium falciparum proliferation | 2011 | Science (New York, N.Y.), Aug-05, Volume: 333, Issue:6043 | Chemical genomic profiling for antimalarial therapies, response signatures, and molecular targets. |
| AID1346987 | P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1346986 | P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen | 2019 | Molecular pharmacology, 11, Volume: 96, Issue:5 | A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein. |
| AID1347151 | Optimization of GU AMC qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay | 2020 | Proceedings 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. |
| AID1347410 | qHTS for inhibitors of adenylyl cyclases using a fission yeast platform: a pilot screen against the NCATS LOPAC library | 2019 | Cellular signalling, 08, Volume: 60 | A fission yeast platform for heterologous expression of mammalian adenylyl cyclases and high throughput screening. |
| AID1347405 | qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS LOPAC collection | 2020 | ACS 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. |
| AID1347059 | CD47-SIRPalpha protein protein interaction - Alpha assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347058 | CD47-SIRPalpha protein protein interaction - HTRF assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1347057 | CD47-SIRPalpha protein protein interaction - LANCE assay qHTS validation | 2019 | PloS one, , Volume: 14, Issue:7 | Quantitative high-throughput screening assays for the discovery and development of SIRPα-CD47 interaction inhibitors. |
| AID1346211 | Human aldo-keto reductase family 1 member B (1.-.-.- Oxidoreductases) | 2000 | Journal 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. |
| AID1797505 | In 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)- | 2003 | Journal 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. |
| AID1802103 | IC50-Activity Assay (AR) from Article 10.1021/acschembio.6b00382: \\IDD388 Polyhalogenated Derivatives as Probes for an Improved Structure-Based Selectivity of AKR1B10 Inhibitors\\ | |||
| AID1794808 | Fluorescence-based screening to identify small molecule inhibitors of Plasmodium falciparum apicoplast DNA polymerase (Pf-apPOL). | 2014 | Journal of biomolecular screening, Jul, Volume: 19, Issue:6 | A High-Throughput Assay to Identify Inhibitors of the Apicoplast DNA Polymerase from Plasmodium falciparum. |
| AID1794808 | Fluorescence-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] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 203 (41.86) | 18.7374 |
| 1990's | 152 (31.34) | 18.2507 |
| 2000's | 75 (15.46) | 29.6817 |
| 2010's | 43 (8.87) | 24.3611 |
| 2020's | 12 (2.47) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (27.63) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 44 (8.80%) | 5.53% |
| Reviews | 29 (5.80%) | 6.00% |
| Case Studies | 3 (0.60%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 424 (84.80%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||