English A R, Retsema J A, Lynch J E
Antimicrob Agents Chemother. 1976 Jul;10(1):132-8. doi: 10.1128/AAC.10.1.132.
In the new agent 3-(5-tetrazolyl)penam, hereafter referred to as CP-35,587, the carboxyl function at C3 in the penicillin nucleus has been replaced with the 5-tetrazolyl moiety. Marked changes in spectrum and resistance to gram-negative beta-lactamases, particularly with regard to Klebsiella pneumoniae isolates, were conferred by this modification. The anti-Klebsiella activity clearly distinguishes the antibacterial spectrum of CP-35,587 from any known broad-spectrum penicillin. Compared to orally active cephalosporins, the spectrum advantage of CP-35,587 encompasses Enterobacter, Serratia marcescens, Citrobacter, Providencia, Haemophilus influenzae, and Streptococcus faecalis, both in vitro and in murine infections produced by many of the above-named microorganisms. Thus, CP-35,587 combines and extends the antibacterial activity of broad-spectrum penicillins and orally active cephalosporins.
在新型药物3-(5-四氮唑基)青霉烷（以下简称CP-35587）中，青霉素母核C3位的羧基官能团已被5-四氮唑基部分取代。这一修饰使光谱以及对革兰氏阴性β-内酰胺酶的抗性发生了显著变化，尤其是对于肺炎克雷伯菌分离株而言。这种抗肺炎克雷伯菌活性使CP-35587的抗菌谱明显有别于任何已知的广谱青霉素。与口服活性头孢菌素相比，CP-35587的光谱优势在体外以及在由上述多种微生物引起的小鼠感染中均涵盖了肠杆菌属、粘质沙雷氏菌、柠檬酸杆菌属、普罗威登斯菌属、流感嗜血杆菌和粪肠球菌。因此，CP-35587兼具并扩展了广谱青霉素和口服活性头孢菌素的抗菌活性。
