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青霉素与头孢菌素类抗生素作为化学治疗剂的历史各达40年及20年之久。这类药物是细菌特有的细胞壁胞壁质的合成抑制剂,所以是对人体细胞没有作用点的选择毒性好的药物,迄今为止仍被广泛地应用于临床。另外,在临床上分离的许多耐药性菌株,由于产生β-内酰胺酶,因此合成了许多对β-内酰胺酶稳定的衍生物。由于上述原困,β-内酰胺类抗生素对其抗菌活性、抗菌谱、耐药菌的对策、体内动态等方面加以改进,最近又发现了青霉素、头孢菌素以外的新品种。这些品种是研究β-内酰胺抗生素的结构与抗菌活性之间的关系的最合适的材料。
The history of penicillin and cephalosporin antibiotics as chemotherapeutic agents has been around for 40 years and 20 years. These drugs are bacterial cell wall parenchyma synthesis inhibitor, so it has no effect on human cells selective toxicity drugs, so far has been widely used in clinical. In addition, many drug-resistant strains that are clinically isolated, due to the production of β-lactamase, have synthesized a number of β-lactamase-stable derivatives. As the original sleepy, β-lactam antibiotics on its antibacterial activity, antibacterial spectrum, drug-resistant bacteria to countermeasures, such as in vivo dynamics to be improved, recently discovered penicillin, cephalosporins other than new varieties. These varieties are the most suitable materials for studying the relationship between the structure and the antibacterial activity of the? -lactam antibiotic.