三唑头孢菌素衍生物的合成及其抗菌活性

Synthesis and Antimicrobial Activity of Triazolylcepha-losporins

以青霉素G的扩环产物7-苯乙酰氨基-3-甲基-3-头孢烯-4-羧酸为起始原料,合成了13个3′位上有4,5-双取代-V-三唑基的未见文献报道的头孢菌素衍生物,经元素分析及光谱数据确证其结构。体外抑菌试验结果表明,其中7个化合物(9a～g)具有较强的广谱抗菌活性。

Using 7-phenylacetamido-3-methyl-3-cephem-4-carboxylic acid as starting material, a series of cephalosporins bearing 4, 5-disubstituted-V-triazolyl groups on the C-3' position of cephem nucleus were synthesized. Their structures were determined by elemental analyses, infrared spectra and nuclear magnetic resonance spectra. Minimum Inhibitory Concentration (MIC) values in vitro showed that compounds 9a～g possessed higher activities against both Gram-positive and Gram-negative bacteria.