7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors.

Eugene B Grant,Barbara D Foleno,Raul Goldschmidt,Jamese J Hilliard,Shu-Chen Lin,Brian Morrow,Steven D Paget,Michele A Weidner-Wells,Xiaodong Xu,Xiaoqing Xu,William V Murray,Karen Bush,Mark J Macielag

Bioorganic & Medicinal Chemistry Letters（2014）

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摘要

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.

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关键词

Antibacterial agent,Fluoroquinolone-resistant,Alkylidenylpiperidinyl fragment

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