7-(4-Alkylidenylpiperidinyl)-quinolone bacterial topoisomerase inhibitors.
Grant EB, Foleno BD, Goldschmidt R, Hilliard JJ, Lin SC, Morrow B, Paget SD, Weidner-Wells MA, Xu X, Xu X, Murray WV, Bush K, Macielag MJ.
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.