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具有酰化的芳甘氨酰侧链的青霉素和头孢菌素如a、b、c、d等式均具有抗绿脓杆菌作用,对绿脓杆菌菌膜上所存在的青霉素结合蛋白-3(PBP_3)有较高的亲和力,影响细菌细胞隔膜的形成,使细菌形态变为长丝状而失活~[1]。国产呋脲苄青霉素钠盐(BLP-1597)经体外抗菌试验,药理、临床证实,虽对β-内酰胺酶不稳定,但体外抗绿脓杆菌作用,却优于羧苄青霉素,临床治疗中,对阴性杆菌感染较为满意。为此我们合成了呋脲苄头孢菌素Ⅲ＇a～c及其(S)-亚砜Ⅳ＇a-c和砜V＇a-b等衍生物,并进行了体外抗菌活性比较试验。
Penicillins and cephalosporins with acylated arylglycyl side chains, such as a, b, c, d, all have anti-Pseudomonas aeruginosa activity against penicillin-binding protein-3 PBP_3) has a higher affinity, affecting the formation of bacterial cell membrane, so that the filamentous bacteria in the form of inactivation ~ [1]. The domestic furosemide penicillin sodium salt (BLP-1597) in vitro antibacterial test, pharmacological and clinical evidence, although the β-lactamase instability, but in vitro anti-Pseudomonas aeruginosa effect, but better than carbenicillin, clinical treatment , More satisfied with negative bacilli infection. For this purpose, we synthesized furfuralbacillin Ⅲ’a ~ c and its (S) -sulfoxide Ⅳ’a-c and sulfone V’a-b and other derivatives, and in vitro antibacterial activity comparison test.