4-甲基化头孢菌素类化合物的合成和生物活性

Synthesis and biological activity of 4-methylcephalosporin compounds

为了寻找具有较好抗菌活性的新型头孢菌素,设计并合成一系列2-位甲基化头孢菌素类化合物,经结构确证发现反应产物不是预期的2-位甲基取代的头孢菌素,而是新结构的4-位甲基化头孢烯类化合物。所合成的2个4-甲基化头孢烯类化合物的结构经核磁共振谱、质谱和元素分析确认,并采用抑菌试验测定了该二化合物,结果表明其可作为β-内酰胺酶抑制剂的先导物开展进一步研究。

In order to find new cephalosporin derivaties, a series of 2- substituted cephalosporins compounds were designed and synthesized. Spectrum analysis methods were used to ascertain the structure of the new compounds, it shown that the new compounds were not 2-substituted but 4-substituted cephalosporins. The structures of these two new compounds were confirmed by ^1H-NMR, MS and elemental analysis. Antibacterial activities of the 4-substituted compounds on standard bacteria were determined. The results show that they are worth of further studies as lead compound of β- lactamase inhibitor.