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  • Title: Synthesis and biological evaluation of irreversible inhibitors of aldose reductase.
    Author: Ares JJ, Kador PF, Miller DD.
    Journal: J Med Chem; 1986 Nov; 29(11):2384-9. PubMed ID: 3097318.
    Abstract:
    5-Isothiocyanatoalrestatin (1b) and 5-azidoalrestatin (1c) were prepared synthetically and examined as potential affinity and photoaffinity inhibitors of rat lens aldose reductase. Both compound 1b and 1c under appropriate conditions at 10(-4) M 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.
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