title: 3-aminoquinazolinediones as a new class of antibacterial agents demonstrating excellent antibacterial activity against wild-type and multidrug resistant organisms.
abstract: The 3-aminoquinzolinediones represent a new series of antibacterial agents structurally related to the fluoroquinolones. They are inhibitors of bacterial gyrase and topoisomerase IV and demonstrate clinically useful antibacterial activity against fastidious Gram-negative and Gram-positive organisms, including multidrug- and fluoroquinolone-resistant organisms. These agents also demonstrate in vivo efficacy in murine systemic infection models.
authors.affiliation: Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. edmund.ellsworth@pfizer.com
authors.forename: Edmund L
authors.initials: EL
authors.lastname: Ellsworth
authors.forename: Tuan P
authors.initials: TP
authors.lastname: Tran
authors.forename: H D Hollis
authors.initials: HD
authors.lastname: Showalter
authors.forename: Joseph P
authors.initials: JP
authors.lastname: Sanchez
authors.forename: Brian M
authors.initials: BM
authors.lastname: Watson
authors.forename: Michael A
authors.initials: MA
authors.lastname: Stier
authors.forename: John M
authors.initials: JM
authors.lastname: Domagala
authors.forename: Stephen J
authors.initials: SJ
authors.lastname: Gracheck
authors.forename: E Themis
authors.initials: ET
authors.lastname: Joannides
authors.forename: Martin A
authors.initials: MA
authors.lastname: Shapiro
authors.forename: Steve A
authors.initials: SA
authors.lastname: Dunham
authors.forename: Debra L
authors.initials: DL
authors.lastname: Hanna
authors.forename: Michael D
authors.initials: MD
authors.lastname: Huband
authors.forename: Jeffrey W
authors.initials: JW
authors.lastname: Gage
authors.forename: Joel C
authors.initials: JC
authors.lastname: Bronstein
authors.forename: Jia Yeu
authors.initials: JY
authors.lastname: Liu
authors.forename: Dai Q
authors.initials: DQ
authors.lastname: Nguyen
authors.forename: Rajeshwar
authors.initials: R
authors.lastname: Singh
mesh_terms: D000900:Anti-Bacterial Agents / Q000138:chemical synthesis* / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects*; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors; D024901:Drug Resistance, Multiple, Bacterial / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D006090:Gram-Negative Bacteria / Q000187:drug effects; D006094:Gram-Positive Bacteria / Q000187:drug effects; D016106:Methicillin Resistance; D008826:Microbial Sensitivity Tests; D052999:Quinazolinones / Q000138:chemical synthesis*; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D052999:Quinazolinones; D059005:Topoisomerase II Inhibitors; D027101:DNA Topoisomerase IV