Watanabe N, Katsu K, Moriyama M, Kitoh K
Department of Microbiology, Tsukuba Research Laboratories, Eisai Co. Ltd., Ibaraki, Japan.
Antimicrob Agents Chemother. 1988 May;32(5):693-701. doi: 10.1128/AAC.32.5.693.
E1040 is a new parenteral cephalosporin with a broad antibacterial spectrum and potent antipseudomonal activity. The compound was four- to eightfold more active than ceftazidime and cefsulodin against Pseudomonas aeruginosa (MIC of E1040 for 90% of strains tested [MIC90], 3.13 micrograms/ml). E1040 also showed a potent activity against other glucose-nonfermentative rods, including Acinetobacter species. The activities of E1040 against most species of the family Enterobacteriaceae were roughly comparable to the activities of ceftazidime and cefmenoxime and exceeded that of cefotiam. Against Citrobacter freundii (MIC90, 0.78 micrograms/ml), Enterobacter cloacae (MIC90, 3.13 micrograms/ml), and Enterobacter aerogenes (MIC90, 0.2 micrograms/ml), E1040 was 16- to 256-fold more active than ceftazidime and cefmenoxime. The activities of E1040 against gram-positive cocci and anaerobes were comparable to those of ceftazidime, but the compound was less active than cefmenoxime. E1040 was at least as resistant as ceftazidime and cefmenoxime to hydrolysis by various beta-lactamases and showed high affinities for penicillin-binding protein 3 of both Escherichia coli and P. aeruginosa.
E1040是一种新型胃肠外头孢菌素，具有广谱抗菌活性和强大的抗假单胞菌活性。该化合物对铜绿假单胞菌的活性比头孢他啶和头孢磺啶高4至8倍（E1040对90%受试菌株的最低抑菌浓度[MIC90]为3.13微克/毫升）。E1040对包括不动杆菌属在内的其他非发酵葡萄糖杆菌也显示出强大活性。E1040对大多数肠杆菌科细菌的活性大致与头孢他啶和头孢甲肟相当，且超过头孢替安。针对弗氏柠檬酸杆菌（MIC90为0.78微克/毫升）、阴沟肠杆菌（MIC90为3.13微克/毫升）和气生性肠杆菌（MIC90为0.2微克/毫升），E1040的活性比头孢他啶和头孢甲肟高16至256倍。E104对革兰氏阳性球菌和厌氧菌的活性与头孢他啶相当，但该化合物的活性低于头孢甲肟。E1040对各种β-内酰胺酶水解的耐药性至少与头孢他啶和头孢甲肟相同，并且对大肠杆菌和铜绿假单胞菌的青霉素结合蛋白3具有高亲和力。
