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  • Title: Structure-activity relationships studies of quinoxalinone derivatives as aldose reductase inhibitors.
    Author: Hussain S, Parveen S, Hao X, Zhang S, Wang W, Qin X, Yang Y, Chen X, Zhu S, Zhu C, Ma B.
    Journal: Eur J Med Chem; 2014 Jun 10; 80():383-92. PubMed ID: 24793885.
    Abstract:
    Novel quinoxalinone derivatives were synthesized and tested for their inhibitory activity against aldose reductase. Among them, N1-acetate derivatives had significant activity in a range of IC50 values from low micromolar to submicromolar, and compound 15a bearing a C3-phenethyl side chain was identified as the most potent inhibitor with an IC50 value of 0.143 μM. The structure-activity studies suggested that both C3-phenethyl and C6-NO2 groups play an important role in enhancing the activity and selectivity of the quinoxalinone based inhibitors.
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