title: Novel quinoline derivatives as inhibitors of bacterial DNA gyrase and topoisomerase IV.
abstract: A structurally novel set of inhibitors of bacterial type II topoisomerases with potent in vitro and in vivo antibacterial activity was developed. Dual-targeting ability, hERG inhibition, and pharmacokinetic properties were also assessed.
authors.affiliation: Pfizer Worldwide Research and Development, Eastern Point Road, Groton, CT 06340, USA. mjmitton@owu.edu
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Mitton-Fry
authors.forename: Steven J
authors.initials: SJ
authors.lastname: Brickner
authors.forename: Judith C
authors.initials: JC
authors.lastname: Hamel
authors.forename: Lori
authors.initials: L
authors.lastname: Brennan
authors.forename: Jeffrey M
authors.initials: JM
authors.lastname: Casavant
authors.forename: Michael
authors.initials: M
authors.lastname: Chen
authors.forename: Tao
authors.initials: T
authors.lastname: Chen
authors.forename: Xiaoyuan
authors.initials: X
authors.lastname: Ding
authors.forename: James
authors.initials: J
authors.lastname: Driscoll
authors.forename: Joel
authors.initials: J
authors.lastname: Hardink
authors.forename: Thuy
authors.initials: T
authors.lastname: Hoang
authors.forename: Erbing
authors.initials: E
authors.lastname: Hua
authors.forename: Michael D
authors.initials: MD
authors.lastname: Huband
authors.forename: Meghan
authors.initials: M
authors.lastname: Maloney
authors.forename: Anthony
authors.initials: A
authors.lastname: Marfat
authors.forename: Sandra P
authors.initials: SP
authors.lastname: McCurdy
authors.forename: Dale
authors.initials: D
authors.lastname: McLeod
authors.forename: Michael
authors.initials: M
authors.lastname: Plotkin
authors.forename: Usa
authors.initials: U
authors.lastname: Reilly
authors.forename: Shaughn
authors.initials: S
authors.lastname: Robinson
authors.forename: John
authors.initials: J
authors.lastname: Schafer
authors.forename: Richard M
authors.initials: RM
authors.lastname: Shepard
authors.forename: James F
authors.initials: JF
authors.lastname: Smith
authors.forename: Gregory G
authors.initials: GG
authors.lastname: Stone
authors.forename: Chakrapani
authors.initials: C
authors.lastname: Subramanyam
authors.forename: Kwansik
authors.initials: K
authors.lastname: Yoon
authors.forename: Wei
authors.initials: W
authors.lastname: Yuan
authors.forename: Richard P
authors.initials: RP
authors.lastname: Zaniewski
authors.forename: Christopher
authors.initials: C
authors.lastname: Zook
mesh_terms: D000818:Animals; D000900:Anti-Bacterial Agents / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D027081:DNA Gyrase / Q000378:metabolism; D027101:DNA Topoisomerase IV / Q000037:antagonists & inhibitors* / Q000378:metabolism; D004250:DNA Topoisomerases, Type II / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D004791:Enzyme Inhibitors / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051638:Ether-A-Go-Go Potassium Channels / Q000037:antagonists & inhibitors; D006801:Humans; D008826:Microbial Sensitivity Tests; D015394:Molecular Structure; D011804:Quinolines / Q000008:administration & dosage / Q000737:chemistry / Q000494:pharmacology*; D051381:Rats; D013211:Staphylococcus aureus / Q000187:drug effects* / Q000201:enzymology; D013296:Streptococcus pneumoniae / Q000187:drug effects* / Q000201:enzymology; D013329:Structure-Activity Relationship; D059005:Topoisomerase II Inhibitors
chemical_list: D000900:Anti-Bacterial Agents; D004791:Enzyme Inhibitors; D051638:Ether-A-Go-Go Potassium Channels; D011804:Quinolines; D059005:Topoisomerase II Inhibitors; C037219:quinoline; D027101:DNA Topoisomerase IV; D027081:DNA Gyrase; D004250:DNA Topoisomerases, Type II