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  • Title: Structure-activity relationships of 3-aminoquinazolinediones, a new class of bacterial type-2 topoisomerase (DNA gyrase and topo IV) inhibitors.
    Author: Tran TP, Ellsworth EL, Sanchez JP, Watson BM, Stier MA, Showalter HD, Domagala JM, Shapiro MA, Joannides ET, Gracheck SJ, Nguyen DQ, Bird P, Yip J, Sharadendu A, Ha C, Ramezani S, Wu X, Singh R.
    Journal: Bioorg Med Chem Lett; 2007 Mar 01; 17(5):1312-20. PubMed ID: 17196390.
    Abstract:
    A series of 3-aminoquinazolinediones was synthesized and evaluated for its antibacterial and DNA gyrase activity. The SAR around the quinazolinedione core was explored and the optimal substitutions were combined to give two compounds, 2r and 2s, with exceptional enzyme potency (IC50 = 0.2 microM) and activity against gram-positive organisms (MIC's = 0.015-0.06 microg/mL).
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