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现在对感染症最广泛使用β-内酰胺类抗生素的主要耐药性机理,是由于细胞外膜的非通透性和细菌产生的钝化酶(主要是β-内酰胺酶)而失去活性的。所以新的β-内酰胺药物研制的方向主要是对各种菌种的细胞外膜通透性要好,抗菌谱要广,并对细菌产生的β-内酰胺酶有耐酶性,保持β-内酰胺环,其目的是增强抗菌活性。在β-内酰胺酶中,分解青霉素类的为青霉素酶,分解头孢菌素的为头孢菌素酶。
The main mechanism of resistance to β-lactam antibiotics, which are now most widely used in infectious diseases, is due to the inactivation of extracellular membrane impermeability and bacterial inactivation enzymes (mainly β-lactamases) . Therefore, the development of new β-lactam drug is mainly for the various cell species of the outer membrane permeability is better antibacterial spectrum to a wide range of bacteria and bacteria resistant to β-lactamase, β- Lactam ring, the purpose of which is to enhance antibacterial activity. In the β-lactamase, the decomposition of penicillin for penicillinase, cephalosporin decomposition cephalosporinase.