论文部分内容阅读
最近几年,有许多新的β-内酰胺抗生素应用于临床。这些抗生素中包括一些特别有价值的碳青霉烯类。牛链霉菌产生的具有广泛抗菌谱及很强的抗革兰氏阳性菌、阴性菌活性的硫霉素(Thienamycin)的发现,开辟了β-内酰胺抗生素的新纪元。后来又发现了一些碳青霉烯,如橄榄酸、Carpetimycins、Asparenomycins 等等,并对它们中的某些物质进行了化学改造。然而,除 Imipenem(N-亚胺甲基硫霉素)外,还没有一个有效地用于临床。Imipenem 和其它相关的碳青霉烯易被肾脱氢肽酶(DHP-1)所钝化,但与一种特异的 DHP-1抑制剂(Cilastatin 联合给药后克服了 Imipenem 的这种不稳定性。这种联合给药已用于治疗各种感染。住友制药公司与 ICI 制药集团联合在世界范围内进行
In recent years, there are many new β-lactam antibiotics used clinically. Some of these antibiotics include particularly valuable carbapenems. The discovery of Thienamycin, a broad antimicrobial spectrum produced by Streptomyces bovinus and active against Gram-positive and -negative bacteria, opens up a new era of beta-lactam antibiotics. Later, some carbapenems were found, such as olive acid, Carpetimycins, Asparenomycins and so on, and some of them were chemically modified. However, none of them has been effectively used in clinical practice except Imipenem (N-imine methylthiomycin). Imipenem and other related carbapenems are readily deactivated by the renin dehydropeptidase (DHP-1) but overcome this instability of Imipenem after co-administration with a specific DHP-1 inhibitor (Cilastatin) This co-administration has been used to treat various infections. Sumitomo Pharmaceuticals and ICI Pharmaceutical Group jointly carried out in the world