Bioorganic and Medicinal Chemistry Letters p. 4405 - 4409 (2004)
Update date:2022-08-02
Topics:
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
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.
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