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β-内酰胺类抗生素在临床上的广泛应用,导致革兰氏阳性和阴性致病菌耐药现象日趋严重。耐青霉素类的细菌由最初的3/5440株发展到1965年的16.6％,1970年超过80％以上。随耐药性的增强,抗生素用量日益增高,苄青霉素MIC最初为0.02μg/ml,1951年增大为25μg/ml,现已分离得到MIC为2000μg/ml的菌株。许多学者认为革兰氏阳性和阴性菌产生的β-内酰胺酶水解β-内酰胺抗生素,导致耐药性的形成。为此。各国药物工作者进行新抗生素的筛选或化学结构改造,以寻找新广谱抗生素,既耐酶的水解作用,又具强的抗菌活性。此外,针对β-内酰胺类抗生素耐药机理寻找β-内酰胺酶
β-lactam antibiotics widely used in clinical practice, leading to Gram-positive and negative pathogens become increasingly serious drug-resistant. Penicillin-resistant bacteria grew from the first 3/5440 strains to 16.6% in 1965 and more than 80% in 1970. With the increase of antibiotic resistance, the dosage of antibiotics increased day by day. The MIC of penicillin was 0.02μg / ml initially and 25μg / ml in 1951, and the MIC of 2000μg / ml was isolated. Many scholars believe that the β-lactamase produced by Gram-positive and -negative bacteria hydrolyzes β-lactam antibiotics, resulting in the formation of drug resistance. to this end. National drug workers to carry out screening of new antibiotics or chemical structural transformation in search of new broad-spectrum antibiotics, both resistant to enzymatic hydrolysis, but also has strong antibacterial activity. In addition, β-lactamase is searched for the mechanism of β-lactam antibiotic resistance