Verbist L, Verhaegen J
Antimicrob Agents Chemother. 1981 Mar;19(3):402-6. doi: 10.1128/AAC.19.3.402.
The in vitro activity of N-formimidoyl thienamycin (N-f-thienamycin) was compared with the activities of other B-lactam antibiotics, using over 500 clinical bacterial isolates. N-f-Thienamycin inhibited 90% of the isolates of the common Enterobacteriaceae between 0.006 and 2 microgram/ml, regardless of their resistance to amoxicillin, ticarcillin, or cephalothin. It was, however, fourfold less active than moxalactam and ceftazidime and eightfold less active than cefotaxime. N-f-Thienamycin was nearly as active as ceftazidime against Pseudomonas aeruginosa (mean minimal inhibitory concentration, 3.0 microgram/ml) and eightfold more active than cefotaxime and moxalactam. In contrast to cefotaxime, moxalactam, and ceftazidime, N-f-thienamycin was highly active against enterococci (mean minimal inhibitory concentration, 1.3 microgram/ml) and staphylococci. The oxacillin-susceptible Staphylococcus aureus were inhibited between 0.03 and 0.12 microgram/ml, and the oxacillin-resistant S. aureus were inhibited between 0.12 and 2 microgram/ml. The high activity of N-f-thienamycin against both of the most important gram-positive and gram-negative organisms makes it a very promising new antibiotic.
使用500多株临床分离细菌，比较了N-甲脒硫霉素（N-f-硫霉素）与其他β-内酰胺类抗生素的体外活性。N-f-硫霉素在0.006至2微克/毫升之间可抑制90%的常见肠杆菌科分离株，无论它们对阿莫西林、替卡西林或头孢噻吩是否耐药。然而，其活性比拉氧头孢和头孢他啶低四倍，比头孢噻肟低八倍。N-f-硫霉素对铜绿假单胞菌的活性与头孢他啶相近（平均最低抑菌浓度为3.0微克/毫升），比头孢噻肟和拉氧头孢高八倍。与头孢噻肟、拉氧头孢和头孢他啶不同，N-f-硫霉素对肠球菌（平均最低抑菌浓度为1.3微克/毫升）和葡萄球菌具有高活性。对苯唑西林敏感的金黄色葡萄球菌在0.03至0.12微克/毫升之间被抑制，对苯唑西林耐药的金黄色葡萄球菌在0.12至2微克/毫升之间被抑制。N-f-硫霉素对最重要的革兰氏阳性和革兰氏阴性菌均具有高活性，使其成为一种非常有前景的新型抗生素。
