761404-23-3Relevant articles and documents
Synthesis and structural-activity relationships of 3-hydroxyquinazoline-2, 4-dione antibacterial agents
Tran, Tuan P.,Ellsworth, Edmund L.,Stier, Michael A.,Domagala, John M.,Hollis Showalter,Gracheck, Stephen J.,Shapiro, Martin A.,Joannides, Themis E.,Singh, Rajeshwar
, p. 4405 - 4409 (2007/10/03)
The synthesis and SAR of the 3-hydroxyquinazoline diones, a novel class of bacterial topoisomerase inhibitors, is reported. 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.