Trager G M, White G W, Zimelis V M, Panwalker A P
Antimicrob Agents Chemother. 1979 Sep;16(3):297-300. doi: 10.1128/AAC.16.3.297.
The in vitro activity of LY-127935, a new beta-lactam antibiotic, was examined by using 370 clinical bacterial strains. In comparison with several other beta-lactam agents, LY-127935 was the most inhibitory against the Enterobacteriaceae. It was remarkably active against multi-drug-resistant strains of Enterobacter spp., Serratia spp., and Pseudomonas aeruginosa. LY-127935 had four- to eightfold greater activity than did cefoxitin against Bacteroides fragilis. Production of beta-lactamase by Enterobacteriaceae did not influence the minimal inhibitory concentration of LY-127935. However, the beta-lactamase-producing strains of B. fragilis and Haemophilus influenzae had generally higher minimal inhibitory concentrations. LY-127935 was the least active agent tested against gram-positive aerobic cocci. Variations in pH, salt content, protein content, or inocula size had little influence on susceptibility to LY-127935. Although combination studies with LY-127935 and gentamicin demonstrated synergy for P. aeruginosa, the rates of killing for the combination and for gentamicin alone were similar.
使用370株临床细菌菌株检测了新型β-内酰胺抗生素LY-127935的体外活性。与其他几种β-内酰胺类药物相比,LY-127935对肠杆菌科细菌的抑制作用最强。它对阴沟肠杆菌、沙雷氏菌属和铜绿假单胞菌的多重耐药菌株具有显著活性。LY-127935对脆弱拟杆菌的活性比对头孢西丁高4至8倍。肠杆菌科细菌产生β-内酰胺酶并不影响LY-127935的最低抑菌浓度。然而,脆弱拟杆菌和流感嗜血杆菌的产β-内酰胺酶菌株通常具有较高的最低抑菌浓度。LY-127935是所测试的对革兰氏阳性需氧球菌活性最低的药物。pH值、盐含量、蛋白质含量或接种量的变化对LY-127935的敏感性影响很小。虽然LY-127935与庆大霉素的联合研究显示对铜绿假单胞菌有协同作用,但联合用药和单独使用庆大霉素的杀菌率相似。