title: 7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors.
abstract: Novel antibacterial fluoroquinolone agents bearing a 4-alkylidenylpiperidine 7-position substituent are active against quinolone-susceptible and quinolone-resistant gram-positive bacteria, including Streptococcus pneumoniae and MRSA. Analogs 22b, 23c, and 24 demonstrated superior in vitro and in vivo efficacy to ciprofloxacin against these cocci.
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Eugene B
authors.initials: EB
authors.lastname: Grant
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Barbara D
authors.initials: BD
authors.lastname: Foleno
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Raul
authors.initials: R
authors.lastname: Goldschmidt
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Jamese J
authors.initials: JJ
authors.lastname: Hilliard
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Shu-Chen
authors.initials: SC
authors.lastname: Lin
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Brian
authors.initials: B
authors.lastname: Morrow
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Steven D
authors.initials: SD
authors.lastname: Paget
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Michele A
authors.initials: MA
authors.lastname: Weidner-Wells
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Xiaodong
authors.initials: X
authors.lastname: Xu
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Xiaoqing
authors.initials: X
authors.lastname: Xu
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: William V
authors.initials: WV
authors.lastname: Murray
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Karen
authors.initials: K
authors.lastname: Bush
authors.affiliation: Janssen Research & Development, L.L.C., Welsh & McKean Roads, Spring House, PA 19477, USA.
authors.forename: Mark J
authors.initials: MJ
authors.lastname: Macielag
mesh_terms: D000900:Anti-Bacterial Agents / Q000494:pharmacology*; D006094:Gram-Positive Bacteria / Q000187:drug effects*; D006801:Humans; D015363:Quinolones / Q000494:pharmacology*; D059003:Topoisomerase Inhibitors / Q000494:pharmacology*
chemical_list: D000900:Anti-Bacterial Agents; D015363:Quinolones; D059003:Topoisomerase Inhibitors
keywords: Alkylidenylpiperidinyl fragment; Antibacterial agent; Fluoroquinolone-resistant