title: Synthesis and structural-activity relationships of 3-hydroxyquinazoline-2,4-dione antibacterial agents.
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.
authors.affiliation: Department of Chemistry, Pfizer Global Research and Development, Ann Arbor Laboratories, 2800 Plymouth Road, MI 48105, USA. tuan.tran@pfizer.com
authors.forename: Tuan P
authors.initials: TP
authors.lastname: Tran
authors.forename: Edmund L
authors.initials: EL
authors.lastname: Ellsworth
authors.forename: Michael A
authors.initials: MA
authors.lastname: Stier
authors.forename: John M
authors.initials: JM
authors.lastname: Domagala
authors.forename: H D
authors.initials: HD
authors.lastname: Showalter
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Gracheck
authors.forename: Martin A
authors.initials: MA
authors.lastname: Shapiro
authors.forename: Themis E
authors.initials: TE
authors.lastname: Joannides
authors.forename: Rajeshwar
authors.initials: R
authors.lastname: Singh
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis*; D006912:Hydroxyquinolines / Q000138:chemical synthesis; D008826:Microbial Sensitivity Tests / Q000706:statistics & numerical data; D011799:Quinazolines / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship
chemical_list: D000900:Anti-Bacterial Agents; D006912:Hydroxyquinolines; D011799:Quinazolines