In vitro Antibacterial Activities of Novel Fluoroquinolone DWP20367

신합성 플로로퀴놀론계 항생물질인 DWP20367의 In vitro 항균효과

  • 김지연 ((주)대웅제약 중앙연구소) ;
  • 최문정 ((주)대웅제약 중앙연구소) ;
  • 한승희 ((주)대웅제약 중앙연구소) ;
  • 심점순 ((주)대웅제약 중앙연구소) ;
  • 정연의 ((주)대웅제약 중앙연구소) ;
  • 손호정 ((주)대웅제약 중앙연구소) ;
  • 이재욱 ((주)대웅제약 중앙연구소) ;
  • 유영효 ((주)대웅제약 중앙연구소) ;
  • 박명환 ((주)대웅제약 중앙연구소)
  • Published : 1997.04.01

Abstract

The in vitro antibacterial activity of DWP20367 (1-Cyclopropyl-6-fluoro-8-chloro-7-(2,7-diazabicyclo[3,3,0]oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a new broad-spectrum fluoroquinolone, was compared with those of ciprofloxacin (CPFX), sparfloxacin (SPFX) and ofloxacin (OFLX). DWP20367 was showed antibacterial activity much higher than CPFX, SPFX and OFLK against gram-positive bacteria, while it was slightly more superior to quinolones against gram-negative bacteria. DWP20367 was particularly effective against MRSA, and its $MlC_{90}$ against clinical isolates of methicillin-susceptible S. aureus, low methicillin-resistant S. aureus and high methicillin-resistant S. aureus were 0.098, 0.781 and 1.563 micro g/ml, respectively. Against S. pneumoniae, MIC90 of DWP20367 was 2- to 8-fold higher than those of CPFX. With a view of MIC90, DWP20367 showed slightly more potent activity against P. aeruginosa and E. coli isolates than the control quinolones. DWP20367 activity was not affected by inoculum size and medium pH. But addition of $Mg^{2+}, \;Ca^{2+} $Mg2+, Ca2+ or horse serum (25%) decreased its antibacterial activity. DWP20367 was showed rapidly bactericidal activity within 2 to 4 h, and regrowth was not observed even after 24 h incubation at concentrations near the 4-fold of MIC.

Keywords

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