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 (IC 50 = 0.2 μM) and activity against Gram-positive organisms (MIC’s = 0.015–0.06 μ g/mL).
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