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Comparative antimicrobial activity of O-demethylfortimicin A a derivative of fortimicin A.

机译:O-去甲基福替米星A(福瑞霉素A的衍生物)的比较抗菌活性。

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摘要

The in vitro antimicrobial activity of O-demethylfortimicin A (ODMF), a derivative of fortimicin A, was compared with those of fortimicin A and gentamicin against a spectrum of 256 organisms. All three antibiotics were active in low concentrations against all strains of Enterobacteriaceae, Acinetobacter sp., and Staphylococcus aureus, with ODMF most active against Proteus mirabilis, indole-positive Proteus, and Providencia and gentamicin most active against other species. Activity of each of the antibiotics against group D streptococci was poor. The overall activity of ODMF was superior to that of fortimicin A for all groups of organisms examined and was most pronounced, approximately three-fold, against strains of Pseudomonas aeruginosa. Both ODMF and fortimicin A were resistant to the action of several aminoglycoside-inactivating enzymes, with the exception of 3-N-acetyltransferase-I. ODMF and fortimicin A showed similar rapid bactericidal effects at multiples of the minimum inhibitory concentration and equivalent synergistic activity against enterococci when combined with penicillin G. The combination of carbenicillin with ODMF, fortimicin A, or gentamicin was synergistic for approximately 80% of the P. aeruginosa strains tested. Inactivation of ODMF and fortimicin A when combined with carbenicillin in vitro was minimal or absent, whereas gentamicin was substantially inactivated under similar conditions. ODMF, fortimicin A, and gentamicin exhibited protective activity in mice infected with Escherichia coli, Klebsiella pneumoniae, Proteus vulgaris, S. aureus, or P. aeruginosa. Gentamicin was the most active, followed by ODMF and fortimicin A. The superior in vitro activity of ODMF compared with fortimicin A against P. aeruginosa was confirmed in vivo.
机译:比较了Fortimicin A的衍生物O-demethylfortimicin A(ODMF)的体外抗菌活性与fortimicin A和庆大霉素对256种细菌的体外抗菌活性。所有这三种抗生素在低浓度下均对肠杆菌科,不动杆菌属和金黄色葡萄球菌的所有菌株具有活性,其中ODMF对奇异变形杆菌,吲哚阳性变形杆菌,普罗维登西亚和庆大霉素对其他物种最活跃。每种抗生素对D组链球菌的活性均较差。对于所检查的所有生物体,ODMF的总体活性均优于fortimicin A,并且对铜绿假单胞菌的菌株最明显,约为三倍。除了3-N-乙酰基转移酶-I以外,ODMF和福瑞霉素A均对几种氨基糖苷失活酶的作用有抗性。当与青霉素G结合使用时,ODMF和fortimicin A在最小抑菌浓度和对肠球菌的等效协同活性的倍数上显示出相似的快速杀菌效果。羧苄青霉素与ODMF,fortimicin A或庆大霉素的组合对P的约80%具有协同作用。测试了铜绿菌菌株。当与羧苄青霉素在体外联合使用时,ODMF和fortimicin A的灭活作用极小或不存在,而庆大霉素在类似条件下则基本上灭活。 ODMF,福瑞霉素A和庆大霉素在感染大肠杆菌,肺炎克雷伯菌,寻常变形杆菌,金黄色葡萄球菌或铜绿假单胞菌的小鼠中表现出保护活性。庆大霉素最活跃,其次是ODMF和fortimicinA。在体内证实了ODMF与fortimicin A相比对铜绿假单胞菌具有更高的体外活性。

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