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Chemical Compound Review:

Lidorestat 2-[3-[(4,5,7- trifluorobenzothiazol-2...

Synonyms: IDD-676, CHEMBL363387, SureCN419032, AG-E-73177, EML 676, ...

Van Zandt, M.C. et al., Calcutt, N.A. et al.

Calcutt, Freshwater, Mizisin,

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Disease relevance of Lidorestat

The aldose reductase inhibitor IDD 676 (Lidorestat), given from the onset of diabetes, prevented the development of thermal hyperalgesia and also stopped progression to thermal hypoalgesia when delivered in the last 4 weeks of an 8-week period of diabetes [1].
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 [2].

High impact information on Lidorestat

The lead candidate, 3-[(4,5,7-trifluorobenzothiazol-2-yl)methyl]indole-N-acetic acid (lidorestat, 9) inhibits aldose reductase with an IC(50) of 5 nM, while being 5400 times less active against aldehyde reductase, a related enzyme involved in the detoxification of reactive aldehydes [2].

References

Prevention of sensory disorders in diabetic Sprague-Dawley rats by aldose reductase inhibition or treatment with ciliary neurotrophic factor. Calcutt, N.A., Freshwater, J.D., Mizisin, A.P. Diabetologia (2004) [Pubmed]
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. Van Zandt, M.C., Jones, M.L., Gunn, D.E., Geraci, L.S., Jones, J.H., Sawicki, D.R., Sredy, J., Jacot, J.L., Dicioccio, A.T., Petrova, T., Mitschler, A., Podjarny, A.D. J. Med. Chem. (2005) [Pubmed]

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