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庆大霉素B衍生物Sch 21420与阿米卡星、庆大霉素、奈替米星、西索米星和妥布霉素的体外活性比较。

Comparison of in vitro activity of Sch 21420, a gentamicin B derivative, with those of amikacin, gentamicin, netilmicin, sisomicin, and tobramycin.

作者信息

Thornsberry C, Barry A L, Jones R N, Baker C N, Badal R E, Packer R R

出版信息

Antimicrob Agents Chemother. 1980 Aug;18(2):338-45. doi: 10.1128/AAC.18.2.338.

Abstract

Sch 21420 is a new aminoglycoside synthesized from gentamicin B. Susceptibility tests with Sch 21420, amikacin, gentamicin, netilmicin, sisomicin, and tobramycin were performed on a variety of bacterial species including 44 with known mechanisms of resistance to aminoglycosides. Sch 21420 and amikacin had similar effects on all except Haemophilus influenzae and Neisseria species, which were more susceptible to amikacin. Except with some strains of Serratia marcescens, the drugs used were bactericidal. Sch 21420 and amikacin were more stable than the other four aminoglycosides in the presence of the inactivating enzymes produced by some strains. Strains which were very resistant to Sch 21420 and emikacin either were permeability mutants or produced AAC (6')-I inactivating enzyme. The effect of cations on the susceptibilities of these strains to Sch 21420 and amikacin was seen mostly with Pseudomonas aeruginosa and to Sch 21420 with Acinetobacter. Cations did not affect the susceptibilities of other Pseudomonas species, Enterobacteriaceae, Staphylococcus aureus, or Streptococcus faecalis to Sch 21420 or amikacin.

摘要

Sch 21420是一种由庆大霉素B合成的新型氨基糖苷类抗生素。我们对Sch 21420、阿米卡星、庆大霉素、奈替米星、西索米星和妥布霉素进行了药敏试验,受试菌种包括44种已知对氨基糖苷类抗生素耐药机制的细菌。除对流感嗜血杆菌和奈瑟菌属外,Sch 21420和阿米卡星对其他所有菌种的作用相似,而流感嗜血杆菌和奈瑟菌属对阿米卡星更敏感。除了某些粘质沙雷氏菌菌株外,所用药物均具有杀菌作用。在一些菌株产生的灭活酶存在的情况下,Sch 21420和阿米卡星比其他四种氨基糖苷类抗生素更稳定。对Sch 21420和阿米卡星高度耐药的菌株要么是通透性突变体,要么产生AAC(6')-I灭活酶。阳离子对这些菌株对Sch 21420和阿米卡星敏感性的影响主要见于铜绿假单胞菌,对不动杆菌则主要见于Sch 21420。阳离子不影响其他假单胞菌属、肠杆菌科、金黄色葡萄球菌或粪肠球菌对Sch 21420或阿米卡星的敏感性。

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