C7-이환체 구조를 갖는 새로운 플루오르퀴놀론계 항생제의 in vitro와 in vivo 항균작용

• 영문명: In vitro and in vivo Antibacterial Activity of a New Fluoroquinolone Containing C7-bicyclic Structure
• 발행기관: 대한약학회
• 저자명: 한승희(Seung Hee Han) 최문정(Moon Jung Choi) 김지연(Ji Yeon Kim) 김병오(Byung O Kim) 심점순(Jeom Soon Shim) 강진석(Jin Seok Kang) 손호정(Ho Jung Son) 이재욱(Jae Wook Lee) 유영효(Young Hyo Yu) 박명환(Myung Hwan Park)
• 간행물 정보: 『약학회지』제42권 제4호 (1998년), 428~437쪽, 전체 10쪽
• 주제분류: 의약학 > 기타의약학
• 파일형태: PDF
• 발행일자: 1998.08.31

영문 초록

The in vitro and in vivo antibacterial activities of a new fluoroquinolone, DWP20364(1-cyclopropyl-5-amino-6,8-difluoro-7-(2,7-diazabicyclo[3.3.0]oto-4-ene-7-yl)-1,4-di-hydro-4-oxoquinoline-3-carboxylic acid) were evaluated in comparison with those of ciprofloxacin(CPFX), sparfloxacin(SPFX) and ofloxacin(OFLX). DWP20364 was more potent than CPFX and OFLX against Staphylococcus spp., Streptococcus spp. and Enterococcus faecium MD8b and it was similarly or slightly less active than CPFX against Escherichia spp. and Pseudomonas spp.. For MRSA and OFLX resistant strains (Staphylococcus spp.(14),Enterococcus spp.(4), Acinetobacter spp.(2), Pseudomonas spp.(9), Klebsiella spp.(2) and Serratia spp.(6)),DWP20364(MICs for 90% of strains,0.025 and 12.5mcg/ml, respectively) was 4 to 32 folds more potent than SPFX and CPFX. The activity of DWP20364 decreased moderately in the presence of 5mM Mg2+. However, various pHs and the concentrations of various serum had no effect on the activity of DWP20364. DWP20364 possessed a bacteriocidal effect at the 1MIC against gram positive and gram negative strains. The protective effect of DWP20364 against systemic infections in mice caused by S. aureus Smith or S. aureus L2379 was superior to that of CPFX and SPFX but it was less active than that of CPFX against infection by P. aeruginosa E-2.

키워드

DWP20364 MIC Effect of pH and serum Bactericidal effect Protective effect.