Maejima T, Inoue M, Mitsuhashi S
Episome Institute, Gunma, Japan.
Antimicrob Agents Chemother. 1991 Jan;35(1):104-10. doi: 10.1128/AAC.35.1.104.
KP-736, a new cephen antibiotic with a broad antibacterial spectrum and potent antipseudomonal activity, was evaluated for in vitro antibacterial activity in comparison with ceftazidime, cefotaxime, and cefpirome. KP-736 was significantly more active than the test compounds against gram-negative bacteria, including the Pseudomonas group and ceftazidime-, cefotaxime-, or imipenem-resistant strains, but less active against gram-positive bacteria. KP-736 had very high affinities for penicillin-binding protein 3 (PBP 3) of Escherichia coli K-12 and PBP 1A and PBP 3 of Pseudomonas aerugiosa NCTC 10490 and showed potent bactericidal activities against these two strains. It was stable to hydrolysis by penicillinases and cephalosporinases but was slightly hydrolyzed by oxyiminocephalosporinases and type II penicillinase.
KP - 736是一种新型头孢菌素抗生素，具有广谱抗菌活性和强大的抗假单胞菌活性。我们将其与头孢他啶、头孢噻肟和头孢匹罗进行比较，评估了它的体外抗菌活性。与测试化合物相比，KP - 736对革兰氏阴性菌具有显著更高的活性，包括假单胞菌属以及对头孢他啶、头孢噻肟或亚胺培南耐药的菌株，但对革兰氏阳性菌的活性较低。KP - 736对大肠杆菌K - 12的青霉素结合蛋白3（PBP 3）以及铜绿假单胞菌NCTC 10490的PBP 1A和PBP 3具有非常高的亲和力，并对这两种菌株显示出强大的杀菌活性。它对青霉素酶和头孢菌素酶的水解稳定，但会被氧亚氨基头孢菌素酶和II型青霉素酶轻微水解。
