U-87947E, A POTENT QUINOLONE ANTIBACTERIAL AGENT INCORPORATING A BICYCLO[1.1.1]PENT-1-YL (BCP) SUBUNIT

被引:35
作者
BARBACHYN, MR [1 ]
HUTCHINSON, DK [1 ]
TOOPS, DS [1 ]
REID, RJ [1 ]
ZURENKO, GE [1 ]
YAGI, BH [1 ]
SCHAADT, RD [1 ]
ALLISON, JW [1 ]
机构
[1] UPJOHN CO,CANC & INFECT DIS RES,KALAMAZOO,MI 49001
关键词
D O I
10.1016/S0960-894X(01)81251-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Incorporation of a bicyclo[ 1. 1. I]pent-1-yl group at the N-1 position of quinolone antibacterial agents affords compounds with potent activity. One of these analogs, U-87947E, exhibits enhanced activity relative to that of ciprofloxacin against gram-positive aerobic bacteria and anaerobic organisms. Time-kill kinetic studies reveal that U-87947E is exquisitely bactericidal against ciprofloxacin-resistant Staphylococcus aureus.
引用
收藏
页码:671 / 676
页数:6
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