title: In vitro evaluation of ABT-719, a novel DNA gyrase inhibitor.
abstract: ABT-719 (A-86719.1) is the first compound of a new class of novel DNA gyrase inhibitors, the 2-pyridones, with potent antibacterial activity against gram-positive, gram-negative, and anaerobic organisms. ABT-719 was more active than ciprofloxacin, sparfloxacin, and clinafloxacin against gram-positive bacteria. ABT-719 was particularly active against Staphylococcus aureus (MIC at which 90% of the isolates were inhibited [MIC90] = 0.015 micrograms/ml) and Streptococcus pneumoniae (MIC90 = 0.03 micrograms/ml). ABT-719 was also the most active of the compounds tested against ciprofloxacin-resistant S. aureus isolates, with an MIC90 of 0.25 micrograms/ml, compared with 64 micrograms/ml for ciprofloxacin. Against gram-negative organisms, ABT-719 was as active as or slightly more active than ciprofloxacin and was the most active compound against ciprofloxacin-resistant Pseudomonas aeruginosa (MIC90 = 2.0 micrograms/ml). ABT-719 was also the most active compound against both gram-positive and gram-negative anaerobes, with MIC90s ranging from 0.12 to 0.25 micrograms/ml.
authors.affiliation: Department 47T, Abbott Laboratories, Abbott Park, Illinois 60064-3500, USA.
authors.forename: R K
authors.initials: RK
authors.lastname: Flamm
authors.forename: C
authors.initials: C
authors.lastname: Vojtko
authors.forename: D T
authors.initials: DT
authors.lastname: Chu
authors.forename: Q
authors.initials: Q
authors.lastname: Li
authors.forename: J
authors.initials: J
authors.lastname: Beyer
authors.forename: D
authors.initials: D
authors.lastname: Hensey
authors.forename: N
authors.initials: N
authors.lastname: Ramer
authors.forename: J J
authors.initials: JJ
authors.lastname: Clement
authors.forename: S K
authors.initials: SK
authors.lastname: Tanaka
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D001419:Bacteria / Q000187:drug effects; D008826:Microbial Sensitivity Tests; D011728:Pyridones / Q000494:pharmacology; D059005:Topoisomerase II Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D011728:Pyridones; D059005:Topoisomerase II Inhibitors; C093440:ABT 719