Phenylsulfonylnitromethanes as potent irreversible inhibitors of aldose reductase

Nada H. Saab, Isaac O. Donkor, Libaniel Rodriguez, Peter F. Kador, Duane D. Miller

Research output: Contribution to journalArticlepeer-review

11 Scopus citations

Abstract

Aldose reductase (AR) inhibition provides a viable pharmacologically direct mode for the treatment of diabetic complications. We have synthesized a series of N-4 substituted analogues (15-21) of the known aldose reductase inhibitor phenyl-sulfonylnitromethane. The compounds are potent inhibitors of AR with IC50s between 0.01 and 0.19 μM. Some of the compounds are also potent affinity labels for AR. Compound 19 exhibits the highest and almost complete irreversible inhibition of AR known to date.

Original languageEnglish (US)
Pages (from-to)745-751
Number of pages7
JournalEuropean Journal of Medicinal Chemistry
Volume34
Issue number9
DOIs
StatePublished - Sep 1999

Keywords

  • Aldose reductase
  • Aldose reductase inhibitors
  • Diabetic complication
  • Irreversible inhibitors
  • Phenylsulphonyl- nitromethane

ASJC Scopus subject areas

  • Pharmacology
  • Drug Discovery
  • Organic Chemistry

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