U-87947E, a protein quinolone antibacterial agent incorporating a bicyclo[1.1.1]pent-1-yl (BCP) subunit

Bioorganic & Medicinal Chemistry Letters
1993.0

Abstract

Incorporation of a bicyclo[ 1.1. llpent- l-y1 group at the N- 1 position of quinolone antibacterial agents affords compounds with potent activity. One of these analogs, U-87947& 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 S&&yZococcus uureus.

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