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

…, JM Domagala, HDH Showalter, SJ Gracheck…

Index: 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 Bioorganic and Medicinal Chemistry Letters, 2004 , vol. 14, # 17 p. 4405 - 4409

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Citation Number: 57

Abstract

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.