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在近几年中,各制药公司试图通过在头孢菌素分子中引入新取代基来改善β—内酰胺类有效性和抗菌谱。Rolinson(1986)报道了近期上市头孢菌素类产品是第三代,包括头孢噻肟、头孢三嗪和Ceftazidime,这些头孢菌素在头孢烯环7α位上具有甲氧亚氨基5—氨噻唑部分。上述第三代头孢菌素提高了对β—内酰胺酶稳定性。然而,包括第三代头孢菌素成为迅速发展起来产生质粒编码TEM型β—内酰胺酶突变体的潜在底物,它们对产去阻遏染色体β—内酰胺酶阴沟肠杆菌和绿脓杆菌无效,这对它们在临床上的成功率
In recent years, various pharmaceutical companies have sought to improve the beta-lactam effectiveness and antibacterial spectrum by introducing new substituents into cephalosporin molecules. Rolinson (1986) reported that recently marketed cephalosporins are the third generation, including cefotaxime, cefotaxime and ceftazidime, which have a methoxyimino 5-aminothiazole moiety at the 7 [alpha] . The third generation cephalosporins increase β-lactamase stability. However, the inclusion of third generation cephalosporins has emerged as a potential substrate that has rapidly evolved to produce plasmid-encoded TEM-type beta-lactamase mutants that are ineffective in producing the derepressed chromosomal beta-lactamase Enterobacter cloacae and Pseudomonas aeruginosa, This is their clinical success rate