Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C18H11F3N2O2S |
| Molecular Weight | 376.352 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CN1C=C(CC2=NC3=C(F)C(F)=CC(F)=C3S2)C4=C1C=CC=C4
InChI
InChIKey=KYHVTMFADJNSGS-UHFFFAOYSA-N
InChI=1S/C18H11F3N2O2S/c19-11-6-12(20)18-17(16(11)21)22-14(26-18)5-9-7-23(8-15(24)25)13-4-2-1-3-10(9)13/h1-4,6-7H,5,8H2,(H,24,25)
| Molecular Formula | C18H11F3N2O2S |
| Molecular Weight | 376.352 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
Lidorestat is a highly potent and selective aldose reductase inhibitor with good oral bioavailability that is reported to improve nerve conduction and reduce cataract formation. Lidorestat reduced mortality rates in hAR transgenic mice. Mice receiving lidorestat had similar survival rates as nonhAR-expressing diabetic mice. Lidorestat treatment did not affect plasma lipids, glucose, or weights of diabetic mice. Drugs such as lidorestat will improve human health by reducing the production of toxic products of the polyol pathway. Lidorestat was developed for the treatment of diabetic complications, including neuropathy, retinopathy, cataracts, nephropathy.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| High glucose concentration suppresses a SIRT2 regulated pathway that enhances neurite outgrowth in cultured adult sensory neurons. | 2018-11 |
|
| Updates on Aldose Reductase Inhibitors for Management of Diabetic Complications and Non-diabetic Diseases. | 2016 |
|
| [5-(Benzyloxy)-1H-indol-1-yl]acetic acid, an aldose reductase inhibitor and PPARγ ligand. | 2015 |
|
| Identification of new non-carboxylic acid containing inhibitors of aldose reductase. | 2010-06-01 |
|
| Diabetic cataract-pathogenesis, epidemiology and treatment. | 2010 |
|
| Discovery of [3-(4,5,7-trifluoro-benzothiazol-2-ylmethyl)-pyrrolo[2,3-b]pyridin-1-yl]acetic acids as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. | 2009-04-01 |
|
| Regulation of plasma fructose and mortality in mice by the aldose reductase inhibitor lidorestat. | 2009-02 |
|
| Synthesis, induced-fit docking investigations, and in vitro aldose reductase inhibitory activity of non-carboxylic acid containing 2,4-thiazolidinedione derivatives. | 2008-06-01 |
|
| Discovery of 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat) and congeners as highly potent and selective inhibitors of aldose reductase for treatment of chronic diabetic complications. | 2005-05-05 |
|
| Role of aldose reductase and oxidative damage in diabetes and the consequent potential for therapeutic options. | 2005-05 |
|
| Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor. | 2004-04 |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18974362
Curator's Comment: Mice data
25 mg/kg/day for 6 weeks
Route of Administration:
Oral
| Substance Class |
Chemical
Created
by
admin
on
Edited
Mon Mar 31 18:20:39 GMT 2025
by
admin
on
Mon Mar 31 18:20:39 GMT 2025
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| Record UNII |
R3734K0M7L
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| Record Status |
Validated (UNII)
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C72880
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| Related Record | Type | Details | ||
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SALT/SOLVATE -> PARENT |
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TARGET -> INHIBITOR |
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SOLVATE->ANHYDROUS |
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ACTIVE MOIETY |
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