Synthesis and Biological Evaluation of Irreversible Inhibitors of Aldose Reductase

Jeffrey J. Ares, Duane D. Miller, Peter F. Kador

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

5-Isothiocyanatoalrestatin (lb) and 5-azidoalrestatin (lc) were prepared synthetically and examined as potential affinity and photoaffinity inhibitors of rat lens aldose reductase. Both compound lb and lc under appropriate conditions at 10-4M produced a 70% irreversible inactivation of aldose reductase within 1 min. The enzyme could, in part, be protected by preincubation with sorbinil 2, a known potent inhibitor of aldose reductase.

Original languageEnglish (US)
Pages (from-to)2384-2389
Number of pages6
JournalJournal of Medicinal Chemistry
Volume29
Issue number11
DOIs
StatePublished - 1986

ASJC Scopus subject areas

  • Molecular Medicine
  • Drug Discovery

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