Synthesis and structural-activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents

A series of 3 -hydroxyquinazoline-2,4-diones was synthesized and evaluated for antibacterial activity. This series represents a novel addition to the DNA gyrase inhibitor class of antibacterials. Appropriate substitutions onto the core template yielded compounds with excellent potency against E. coli gyrase and significant in vitro Gram-negative and Gram-positive antibacterial activity. (C) 2004 Elsevier Ltd. All rights reserved.