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微生物细胞能产生破坏青霉素及头孢菌素的β-内酰胺酶,是对该类抗生素耐药的主要原因之一。如果弄清该过程的机理及β-内酰胺酶作为催化剂水解β-内酰胺环的CO-N键的作用,那么,就不难找到可以抑制这些酶活性,并免受其破坏的化合物。目前,根据β-内酰胺梅与其底物分布的关系,可将它们分成三大类,即:青霉素-β-内酰胺酶,头孢菌素-β-内酰胺酶和呋肟头孢菌素-β-内酰胺酶。大肠杆菌、肠杆菌、柠檬酸杆菌、粘质沙雷氏菌、雷氏变形菌、绿脓杆菌所产生的β-内酰胺酶,可以水解苄青霉素、噻孢霉素、唑啉头孢菌素、头孢菌素Ⅳ;与此
Microbial cells can produce damage to penicillin and cephalosporins β-lactamase, is one of the main reasons for the resistance of such antibiotics. If one can understand the mechanism of this process and the action of β-lactamase as a catalyst for the hydrolysis of the CO-N bond of the β-lactam ring, it is not difficult to find compounds that inhibit the activity of these enzymes and protect them from damage. At present, they can be divided into three broad categories based on the distribution of β-lactamase and its substrate: penicillin-β-lactamase, cephalosporin-β-lactamase, and furosemide cephalosporin-β - lactamase. Escherichia coli, Enterobacter, Citrobacter, Serratia marcescens, Proteus marcescens, Pseudomonas aeruginosa produced by β-lactamase, hydrolysis of benzyl penicillin, Cephalosporin IV; with this