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首页> 外文期刊>The Journal of Antibiotics: An International Journal >In Vitro Antibacterial Activity of a New Cephalosporin, FR295389, against IMP-type Metallo-beta-lactamase-producers.
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In Vitro Antibacterial Activity of a New Cephalosporin, FR295389, against IMP-type Metallo-beta-lactamase-producers.

机译:新的头孢菌素FR295389对IMP型金属β-内酰胺酶生产者的体外抗菌活性。

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摘要

FR295389 is a novel dihydroimidazopyrazolium cephalosporin. Although all previously reported cephalosporins had been ineffective against metallo-beta-lactamase (MBL)-producers, FR295389 showed moderate activity against these strains. The MIC values of FR295389 at which 50% and 90% of 21 clinical isolates of IMP-type MBL-producing Pseudomonas aeruginosa were inhibited were 8.0 and 32 mug/ml, respectively. The kinetic study of IMP-1 MBL showed that the K(m) and the k(cat) values against FR295389 were over 20-fold-higher and 12-fold-lower than those against ceftazidime, respectively, suggesting that FR295389 is a poor substrate for IMP-type MBL. This is the first report of a cephalosporin with activity against IMP-type MBL-producers.
机译:FR295389是新型的二氢咪唑并吡唑鎓头孢菌素。尽管以前报道的所有头孢菌素均对金属β-内酰胺酶(MBL)生产者无效,但FR295389对这些菌株显示中等活性。 FR295389的MIC值分别被抑制21个产生IMP的MBL的铜绿假单胞菌临床分离株的50%和90%,其MIC值分别为8.0和32马克/毫升。 IMP-1 MBL的动力学研究表明,抗FR295389的K(m)和k(cat)值分别比抗头孢他啶高20倍和低12倍,这表明FR295389较差IMP型MBL的基材。这是头孢菌素对IMP型MBL产生剂具有活性的首次报道。

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